{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,20]],"date-time":"2026-08-20T14:27:08Z","timestamp":1787236028447,"version":"build-2736575974"},"reference-count":64,"publisher":"Springer Science and Business Media LLC","issue":"1","license":[{"start":{"date-parts":[[2022,10,6]],"date-time":"2022-10-06T00:00:00Z","timestamp":1665014400000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0"},{"start":{"date-parts":[[2022,10,6]],"date-time":"2022-10-06T00:00:00Z","timestamp":1665014400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0"}],"funder":[{"DOI":"10.13039\/501100007950","name":"Tanta University","doi-asserted-by":"crossref","id":[{"id":"10.13039\/501100007950","id-type":"DOI","asserted-by":"crossref"}]}],"content-domain":{"domain":["link.springer.com"],"crossmark-restriction":false},"short-container-title":["Sci Rep"],"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>\n                    Limited presence of hCA IX in normal physiological tissues and their overexpression only in solid hypoxic tumors made this isoform excellent possible target for developing new anticancer agents. We reported designing and synthesis of two novel series of benzenesulfonamides derivatives as hCA IX inhibitors bearing rigid cyclic linkers (1,3,5-dihydrotriazine in series\n                    <jats:bold>A<\/jats:bold>\n                    and 1,3,5-triazine in series\n                    <jats:bold>B<\/jats:bold>\n                    ) in replace of traditional linear linkers. Also, novel cyanoethenyl spacer was assembled next to the 1,3,5-triazine linker in series\n                    <jats:bold>B<\/jats:bold>\n                    . Target compounds of series\n                    <jats:bold>(A)<\/jats:bold>\n                    and\n                    <jats:bold>(B)<\/jats:bold>\n                    were screened against four hCA isoforms. Human CA IX efficiently inhibited in series (\n                    <jats:bold>A<\/jats:bold>\n                    ) by compound\n                    <jats:bold>5a (<\/jats:bold>\n                    K\n                    <jats:sub>I<\/jats:sub>\n                    \u2009=\u2009134.8\u00a0nM). Meanwhile, in series\n                    <jats:bold>(B)<\/jats:bold>\n                    the most active inhibitor was\n                    <jats:bold>12i<\/jats:bold>\n                    (K\n                    <jats:sub>I<\/jats:sub>\n                    \u2009=\u200938.8\u00a0nM). US-NCI protocol was followed to evaluate the anticancer activity of target compounds against panel of sixty cancer cell lines. Compound\n                    <jats:bold>12d,<\/jats:bold>\n                    exposed the best activity towards breast cancer (MDA-MB-468) with GI%\u2009=\u200962%. The most active analogues,\n                    <jats:bold>12d<\/jats:bold>\n                    and\n                    <jats:bold>12i<\/jats:bold>\n                    were further screened for in vitro cytotoxic activity under hypoxic condition against breast cancer (MDA-MB-468) (IC\n                    <jats:sub>50<\/jats:sub>\n                    \u2009=\u20093.99\u2009\u00b1\u20090.21 and 1.48\u2009\u00b1\u20090.08\u00a0\u00b5M, respectively) and leukemia (CCRF-CM) cell line (IC\n                    <jats:sub>50<\/jats:sub>\n                    \u2009=\u20094.51\u2009\u00b1\u20090.24 and 9.83\u2009\u00b1\u20090.52\u00a0\u00b5M, respectively). In addition,\n                    <jats:bold>12d<\/jats:bold>\n                    arrested breast cancer MDA-MB-468 cell cycle in G0-G1 and S phases and induced its apoptosis which indicated by increasing the level of cleaved caspases 3 and 9. Molecular docking was performed for selected analogues to understand their biological alterations. This study revealed that insertion of 1,3,5-triazines as cyclic linkers enhanced the significant anticancer and hCA IX inhibition activity of benzenesulfonamides.\n                  <\/jats:p>","DOI":"10.1038\/s41598-022-21024-7","type":"journal-article","created":{"date-parts":[[2022,10,6]],"date-time":"2022-10-06T12:04:42Z","timestamp":1665057882000},"update-policy":"https:\/\/doi.org\/10.1007\/springer_crossmark_policy","source":"Crossref","is-referenced-by-count":28,"title":["Synthesis and anticancer activity of new benzensulfonamides incorporating s-triazines as cyclic linkers for inhibition of carbonic anhydrase IX"],"prefix":"10.1038","volume":"12","author":[{"given":"Abdelrahman I.","family":"Zain-Alabdeen","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Tarek F.","family":"El-Moselhy","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Nabaweya","family":"Sharafeldin","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Andrea","family":"Angeli","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Claudiu T.","family":"Supuran","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mervat H.","family":"El-Hamamsy","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"297","published-online":{"date-parts":[[2022,10,6]]},"reference":[{"key":"21024_CR1","doi-asserted-by":"publisher","first-page":"229","DOI":"10.3109\/14756366.2013.761876","volume":"28","author":"CT Supuran","year":"2013","unstructured":"Supuran, C. T. Carbonic anhydrases: From biomedical applications of the inhibitors and activators to biotechnological use for CO2 capture. J. Enzyme Inhib. Med. Chem. 28, 229\u2013230 (2013).","journal-title":"J. Enzyme Inhib. Med. Chem."},{"key":"21024_CR2","doi-asserted-by":"publisher","first-page":"2485","DOI":"10.1002\/med.21713","volume":"40","author":"CB Mishra","year":"2020","unstructured":"Mishra, C. B., Tiwari, M. & Supuran, C. T. Progress in the development of human carbonic anhydrase inhibitors and their pharmacological applications: where are we today?. Med. Res. Rev. 40, 2485\u20132565 (2020).","journal-title":"Med. Res. Rev."},{"key":"21024_CR3","doi-asserted-by":"publisher","first-page":"103544","DOI":"10.1016\/j.bioorg.2019.103544","volume":"95","author":"AG Uslu","year":"2020","unstructured":"Uslu, A. G. et al. Benzimidazole derivatives as potent and isoform selective tumor-associated carbonic anhydrase IX\/XII inhibitors. Bioorg. Chem. 95, 103544 (2020).","journal-title":"Bioorg. Chem."},{"key":"21024_CR4","doi-asserted-by":"publisher","first-page":"2555","DOI":"10.1007\/s00784-020-03567-z","volume":"25","author":"ET de Sousa","year":"2021","unstructured":"de Sousa, E. T., Lima-Holanda, A. T., Sales, L. S. & Nobre-dos-Santos, M. Combined effect of starch and sucrose on carbonic anhydrase VI activity in saliva and biofilm of children with early childhood caries. Exposure to starch and sucrose alters carbonic anhydrase VI activity in saliva and biofilm. Clin. Oral Investig. 25, 2555\u20132568 (2021).","journal-title":"Clin. Oral Investig."},{"key":"21024_CR5","doi-asserted-by":"publisher","first-page":"168","DOI":"10.1038\/nrd2467","volume":"7","author":"CT Supuran","year":"2008","unstructured":"Supuran, C. T. Carbonic anhydrases: novel therapeutic applications for inhibitors and activators. Nat. Rev. Drug Discov. 7, 168\u2013181 (2008).","journal-title":"Nat. Rev. Drug Discov."},{"key":"21024_CR6","doi-asserted-by":"publisher","first-page":"713","DOI":"10.1080\/13543776.2018.1519023","volume":"28","author":"CT Supuran","year":"2018","unstructured":"Supuran, C. T. Applications of carbonic anhydrases inhibitors in renal and central nervous system diseases. Expert Opin. Ther. Pat. 28, 713\u2013721 (2018).","journal-title":"Expert Opin. Ther. Pat."},{"key":"21024_CR7","doi-asserted-by":"publisher","first-page":"3317","DOI":"10.1021\/acs.jmedchem.9b02090","volume":"63","author":"M Fares","year":"2020","unstructured":"Fares, M. et al. Discovery of potent dual-tailed benzenesulfonamide inhibitors of human carbonic anhydrases implicated in glaucoma and in vivo profiling of their intraocular pressure-lowering action. J. Med. Chem. 63, 3317\u20133326 (2020).","journal-title":"J. Med. Chem."},{"key":"21024_CR8","doi-asserted-by":"publisher","first-page":"19","DOI":"10.3390\/metabo8010019","volume":"8","author":"MY Mboge","year":"2018","unstructured":"Mboge, M. Y., Mahon, B. P., McKenna, R. & Frost, S. C. Carbonic anhydrases: role in pH control and cancer. Metabolites 8, 19 (2018).","journal-title":"Metabolites"},{"key":"21024_CR9","unstructured":"Pastorek, J. & Pastorekova, S. in Seminars in Cancer Biology. 52\u201364 (Elsevier)."},{"key":"21024_CR10","first-page":"3","volume":"5","author":"MY Mboge","year":"2015","unstructured":"Mboge, M. Y., McKenna, R. & Frost, S. C. Advances in anti-cancer drug development targeting carbonic anhydrase IX and XII. Top. Anti-cancer Res. 5, 3 (2015).","journal-title":"Top. Anti-cancer Res."},{"key":"21024_CR11","doi-asserted-by":"publisher","first-page":"1799","DOI":"10.1002\/med.21497","volume":"38","author":"CT Supuran","year":"2018","unstructured":"Supuran, C. T. et al. Inhibition of carbonic anhydrase IX targets primary tumors, metastases, and cancer stem cells: three for the price of one. Med. Res. Rev. 38, 1799\u20131836 (2018).","journal-title":"Med. Res. Rev."},{"key":"21024_CR12","doi-asserted-by":"publisher","first-page":"48","DOI":"10.3390\/metabo7030048","volume":"7","author":"CT Supuran","year":"2017","unstructured":"Supuran, C. T. Carbonic anhydrase inhibition and the management of hypoxic tumors. Metabolites 7, 48 (2017).","journal-title":"Metabolites"},{"key":"21024_CR13","doi-asserted-by":"publisher","first-page":"729","DOI":"10.1080\/13543776.2018.1508453","volume":"28","author":"A Nocentini","year":"2018","unstructured":"Nocentini, A. & Supuran, C. T. Carbonic anhydrase inhibitors as antitumor\/antimetastatic agents: A patent review (2008\u20132018). Expert Opin. Ther. Pat. 28, 729\u2013740 (2018).","journal-title":"Expert Opin. Ther. Pat."},{"key":"21024_CR14","doi-asserted-by":"publisher","first-page":"404","DOI":"10.1016\/j.bbapap.2009.07.027","volume":"1804","author":"G De Simone","year":"2010","unstructured":"De Simone, G. & Supuran, C. T. Carbonic anhydrase IX: Biochemical and crystallographic characterization of a novel antitumor target. Biochim. Biophys. Acta BBA Proteins Proteom. 1804, 404\u2013409 (2010).","journal-title":"Biochim. Biophys. Acta BBA Proteins Proteom."},{"key":"21024_CR15","doi-asserted-by":"publisher","first-page":"544","DOI":"10.1016\/j.ejmech.2017.12.049","volume":"144","author":"MF Ansari","year":"2018","unstructured":"Ansari, M. F. et al. Design, synthesis and biological evaluation of novel pyridine-thiazolidinone derivatives as anticancer agents: Targeting human carbonic anhydrase IX. Eur. J. Med. Chem. 144, 544\u2013556 (2018).","journal-title":"Eur. J. Med. Chem."},{"key":"21024_CR16","doi-asserted-by":"publisher","first-page":"112923","DOI":"10.1016\/j.ejmech.2020.112923","volume":"209","author":"S Kumar","year":"2021","unstructured":"Kumar, S., Rulhania, S., Jaswal, S. & Monga, V. Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors. Eur. J. Med. Chem. 209, 112923 (2021).","journal-title":"Eur. J. Med. Chem."},{"key":"21024_CR17","doi-asserted-by":"publisher","first-page":"128249","DOI":"10.1016\/j.bmcl.2021.128249","volume":"48","author":"S Manzoor","year":"2021","unstructured":"Manzoor, S., Petreni, A., Raza, M. K., Supuran, C. T. & Hoda, N. Novel triazole-sulfonamide bearing pyrimidine moieties with carbonic anhydrase inhibitory action: Design, synthesis, computational and enzyme inhibition studies. Bioorg. Med. Chem. Lett. 48, 128249 (2021).","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"21024_CR18","doi-asserted-by":"publisher","first-page":"4421","DOI":"10.1021\/cr200176r","volume":"112","author":"V Alterio","year":"2012","unstructured":"Alterio, V., Di Fiore, A., D\u2019Ambrosio, K., Supuran, C. T. & De Simone, G. Multiple binding modes of inhibitors to carbonic anhydrases: how to design specific drugs targeting 15 different isoforms?. Chem. Rev. 112, 4421\u20134468 (2012).","journal-title":"Chem. Rev."},{"key":"21024_CR19","doi-asserted-by":"publisher","first-page":"1896","DOI":"10.1021\/jm101541x","volume":"54","author":"F Pacchiano","year":"2011","unstructured":"Pacchiano, F. et al. Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis. J. Med. Chem. 54, 1896\u20131902 (2011).","journal-title":"J. Med. Chem."},{"key":"21024_CR20","doi-asserted-by":"publisher","first-page":"114008","DOI":"10.1016\/j.ejmech.2021.114008","volume":"228","author":"DM Elimam","year":"2022","unstructured":"Elimam, D. M. et al. Natural inspired ligustrazine-based SLC-0111 analogues as novel carbonic anhydrase inhibitors. Eur. J. Med. Chem. 228, 114008 (2022).","journal-title":"Eur. J. Med. Chem."},{"key":"21024_CR21","doi-asserted-by":"publisher","first-page":"1575","DOI":"10.1080\/14756366.2018.1515933","volume":"33","author":"S Akocak","year":"2018","unstructured":"Akocak, S., Lolak, N., Bua, S. & Supuran, C. T. Discovery of novel 1, 3-diaryltriazene sulfonamides as carbonic anhydrase I, II, VII, and IX inhibitors. J. Enzyme Inhib. Med. Chem. 33, 1575\u20131580 (2018).","journal-title":"J. Enzyme Inhib. Med. Chem."},{"key":"21024_CR22","doi-asserted-by":"publisher","first-page":"1713","DOI":"10.1021\/acs.jmedchem.0c02077","volume":"64","author":"MY Mboge","year":"2021","unstructured":"Mboge, M. Y. et al. Inhibition of carbonic anhydrase using SLC-149: Support for a noncatalytic function of CAIX in breast cancer. J. Med. Chem. 64, 1713\u20131724 (2021).","journal-title":"J. Med. Chem."},{"key":"21024_CR23","doi-asserted-by":"publisher","first-page":"1776","DOI":"10.1016\/j.bmcl.2014.02.030","volume":"24","author":"C Congiu","year":"2014","unstructured":"Congiu, C., Onnis, V., Balboni, G. & Supuran, C. T. Synthesis and carbonic anhydrase I, II, IX and XII inhibition studies of 4-N, N-disubstituted sulfanilamides incorporating 4, 4, 4-trifluoro-3-oxo-but-1-enyl, phenacylthiourea and imidazol-2 (3H)-one\/thione moieties. Bioorg. Med. Chem. Lett. 24, 1776\u20131779 (2014).","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"21024_CR24","doi-asserted-by":"publisher","first-page":"10692","DOI":"10.1021\/acs.jmedchem.6b01389","volume":"59","author":"A Nocentini","year":"2016","unstructured":"Nocentini, A. et al. Benzenesulfonamides incorporating flexible triazole moieties are highly effective carbonic anhydrase inhibitors: synthesis and kinetic, crystallographic, computational, and intraocular pressure lowering investigations. J. Med. Chem. 59, 10692\u201310704 (2016).","journal-title":"J. Med. Chem."},{"key":"21024_CR25","doi-asserted-by":"publisher","first-page":"7015","DOI":"10.1016\/j.tetlet.2014.10.122","volume":"55","author":"H Kothayer","year":"2014","unstructured":"Kothayer, H. et al. Optimised synthesis of diamino-triazinylmethyl benzoates as inhibitors of Rad6B ubiquitin conjugating enzyme. Tetrahedron Lett. 55, 7015\u20137018 (2014).","journal-title":"Tetrahedron Lett."},{"key":"21024_CR26","doi-asserted-by":"publisher","first-page":"117","DOI":"10.1016\/j.bioorg.2018.10.005","volume":"82","author":"N Lolak","year":"2019","unstructured":"Lolak, N., Akocak, S., Bua, S. & Supuran, C. T. Design, synthesis and biological evaluation of novel ureido benzenesulfonamides incorporating 1, 3, 5-triazine moieties as potent carbonic anhydrase IX inhibitors. Bioorg. Chem. 82, 117\u2013122 (2019).","journal-title":"Bioorg. Chem."},{"key":"21024_CR27","doi-asserted-by":"publisher","first-page":"241","DOI":"10.1016\/j.bioorg.2018.08.005","volume":"81","author":"P Miku\u0161","year":"2018","unstructured":"Miku\u0161, P. et al. Novel sulfonamides incorporating 1, 3, 5-triazine and amino acid structural motifs as inhibitors of the physiological carbonic anhydrase isozymes I, II and IV and tumor-associated isozyme IX. Bioorg. Chem. 81, 241\u2013252 (2018).","journal-title":"Bioorg. Chem."},{"key":"21024_CR28","doi-asserted-by":"publisher","first-page":"359","DOI":"10.1016\/j.ijbiomac.2019.07.093","volume":"138","author":"R Ghosh","year":"2019","unstructured":"Ghosh, R., Bharathkar, S. K. & Kishore, N. Anticancer altretamine recognition by bovine serum albumin and its role as inhibitor of fibril formation: Biophysical insights. Int. J. Biol. Macromol. 138, 359\u2013369 (2019).","journal-title":"Int. J. Biol. Macromol."},{"key":"21024_CR29","doi-asserted-by":"publisher","first-page":"62","DOI":"10.1038\/s41375-020-0773-5","volume":"35","author":"P Montesinos","year":"2021","unstructured":"Montesinos, P. et al. Safety and efficacy of talacotuzumab plus decitabine or decitabine alone in patients with acute myeloid leukemia not eligible for chemotherapy: results from a multicenter, randomized, phase 2\/3 study. Leukemia 35, 62\u201374 (2021).","journal-title":"Leukemia"},{"key":"21024_CR30","doi-asserted-by":"publisher","first-page":"1734","DOI":"10.1021\/acs.jmedchem.6b01253","volume":"60","author":"H-L Ng","year":"2017","unstructured":"Ng, H.-L., Ma, X., Chew, E.-H. & Chui, W.-K. Design, synthesis, and biological evaluation of coupled bioactive scaffolds as potential anticancer agents for dual targeting of dihydrofolate reductase and thioredoxin reductase. J. Med. Chem. 60, 1734\u20131745 (2017).","journal-title":"J. Med. Chem."},{"key":"21024_CR31","doi-asserted-by":"publisher","first-page":"5644","DOI":"10.1016\/j.bmcl.2009.08.052","volume":"19","author":"X Ma","year":"2009","unstructured":"Ma, X., Poon, T.-Y., Wong, P. T. H. & Chui, W.-K. Synthesis and in vitro evaluation of 2, 4-diamino-1, 3, 5-triazine derivatives as neuronal voltage-gated sodium channel blockers. Bioorg. Med. Chem. Lett. 19, 5644\u20135647 (2009).","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"21024_CR32","doi-asserted-by":"publisher","first-page":"5428","DOI":"10.1016\/j.bmcl.2011.06.125","volume":"21","author":"X Ma","year":"2011","unstructured":"Ma, X. et al. Synthesis and antimicrobial activity of N1-benzyl or N1-benzyloxy-1, 6-dihydro-1, 3, 5-triazine-2, 4-diamines. Bioorg. Med. Chem. Lett. 21, 5428\u20135431 (2011).","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"21024_CR33","doi-asserted-by":"publisher","first-page":"1616","DOI":"10.3390\/molecules23071616","volume":"23","author":"A Makowska","year":"2018","unstructured":"Makowska, A., S\u0105czewski, F., Bednarski, P. J., S\u0105czewski, J. & Balewski, \u0141. Hybrid molecules composed of 2, 4-diamino-1, 3, 5-triazines and 2-imino-coumarins and coumarins. Synthesis and cytotoxic properties. Molecules 23, 1616 (2018).","journal-title":"Molecules"},{"key":"21024_CR34","doi-asserted-by":"publisher","first-page":"1126","DOI":"10.1248\/cpb.21.1126","volume":"21","author":"M Furukawa","year":"1973","unstructured":"Furukawa, M., Kojima, Y. & Hayashi, S. Reaction of biguanides and related compounds. VII. The condensation of arylbiguanide with \u03b1, \u03b2-unsaturated carboxylic ester in dimethylformamide. Chem. Pharm. Bull. 21, 1126\u20131131 (1973).","journal-title":"Chem. Pharm. Bull."},{"key":"21024_CR35","first-page":"461","volume":"61","author":"E Pomarnacka","year":"2004","unstructured":"Pomarnacka, E., Bednarski, P., Grunert, R. & Reszka, P. Synthesis and anticancer activity of novel 2-amino-4-(4-phenylpiperazino)-1, 3, 5-triazine derivatives. Acta Pol. Pharm. Drug Res 61, 461\u2013467 (2004).","journal-title":"Acta Pol. Pharm. Drug Res"},{"key":"21024_CR36","doi-asserted-by":"publisher","first-page":"219","DOI":"10.1016\/j.ejmech.2005.10.013","volume":"41","author":"F S\u0105czewski","year":"2006","unstructured":"S\u0105czewski, F., Bu\u0142akowska, A., Bednarski, P. & Grunert, R. Synthesis, structure and anticancer activity of novel 2, 4-diamino-1, 3, 5-triazine derivatives. Eur. J. Med. Chem. 41, 219\u2013225 (2006).","journal-title":"Eur. J. Med. Chem."},{"key":"21024_CR37","doi-asserted-by":"publisher","first-page":"2561","DOI":"10.1016\/S0021-9258(18)62326-9","volume":"246","author":"RG Khalifah","year":"1971","unstructured":"Khalifah, R. G. The carbon dioxide hydration activity of carbonic anhydrase: I. Stop-flow kinetic studies on the native human isoenzymes B and C. J. Biol. Chem. 246, 2561\u20132573 (1971).","journal-title":"J. Biol. Chem."},{"key":"21024_CR38","doi-asserted-by":"publisher","first-page":"147","DOI":"10.1016\/j.ejmech.2018.10.068","volume":"162","author":"WM Eldehna","year":"2019","unstructured":"Eldehna, W. M. et al. Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted isatins-SLC-0111 hybrids as carbonic anhydrase inhibitors and antitumor agents. Eur. J. Med. Chem. 162, 147\u2013160 (2019).","journal-title":"Eur. J. Med. Chem."},{"key":"21024_CR39","doi-asserted-by":"publisher","first-page":"49","DOI":"10.1016\/j.ejmech.2018.10.008","volume":"160","author":"MF Abo-Ashour","year":"2018","unstructured":"Abo-Ashour, M. F. et al. Novel indole-thiazolidinone conjugates: Design, synthesis and whole-cell phenotypic evaluation as a novel class of antimicrobial agents. Eur. J. Med. Chem. 160, 49\u201360 (2018).","journal-title":"Eur. J. Med. Chem."},{"key":"21024_CR40","doi-asserted-by":"publisher","first-page":"796","DOI":"10.3109\/14756366.2015.1069288","volume":"31","author":"AA-M Abdel-Aziz","year":"2016","unstructured":"Abdel-Aziz, A.A.-M. et al. Synthesis and potential antitumor activity of 7-(4-substituted piperazin-1-yl)-4-oxoquinolines based on ciprofloxacin and norfloxacin scaffolds: in silico studies. J. Enzyme Inhib. Med. Chem. 31, 796\u2013809 (2016).","journal-title":"J. Enzyme Inhib. Med. Chem."},{"key":"21024_CR41","doi-asserted-by":"publisher","first-page":"113283","DOI":"10.1016\/j.ejmech.2021.113283","volume":"216","author":"M Shaldam","year":"2021","unstructured":"Shaldam, M. et al. Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors. Eur. J. Med. Chem. 216, 113283 (2021).","journal-title":"Eur. J. Med. Chem."},{"key":"21024_CR42","doi-asserted-by":"publisher","first-page":"55","DOI":"10.1016\/0022-1759(83)90303-4","volume":"65","author":"T Mosmann","year":"1983","unstructured":"Mosmann, T. Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays. J. Immunol. Methods 65, 55\u201363 (1983).","journal-title":"J. Immunol. Methods"},{"key":"21024_CR43","doi-asserted-by":"publisher","first-page":"103102","DOI":"10.1016\/j.bioorg.2019.103102","volume":"90","author":"WM Eldehna","year":"2019","unstructured":"Eldehna, W. M. et al. Synthesis, biological evaluation and in silico studies with 4-benzylidene-2-phenyl-5 (4H)-imidazolone-based benzenesulfonamides as novel selective carbonic anhydrase IX inhibitors endowed with anticancer activity. Bioorg. Chem. 90, 103102 (2019).","journal-title":"Bioorg. Chem."},{"key":"21024_CR44","doi-asserted-by":"publisher","first-page":"112019","DOI":"10.1016\/j.ejmech.2019.112019","volume":"189","author":"MA Said","year":"2020","unstructured":"Said, M. A. et al. Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. Eur. J. Med. Chem. 189, 112019 (2020).","journal-title":"Eur. J. Med. Chem."},{"key":"21024_CR45","doi-asserted-by":"publisher","first-page":"518","DOI":"10.1038\/nrm3629","volume":"14","author":"C Bertoli","year":"2013","unstructured":"Bertoli, C., Skotheim, J. M. & De Bruin, R. A. Control of cell cycle transcription during G1 and S phases. Nat. Rev. Mol. Cell Biol. 14, 518\u2013528 (2013).","journal-title":"Nat. Rev. Mol. Cell Biol."},{"key":"21024_CR46","doi-asserted-by":"publisher","first-page":"105451","DOI":"10.1016\/j.bioorg.2021.105451","volume":"117","author":"EM Dokla","year":"2021","unstructured":"Dokla, E. M. et al. Indolin-2-one derivatives as selective Aurora B kinase inhibitors targeting breast cancer. Bioorg. Chem. 117, 105451 (2021).","journal-title":"Bioorg. Chem."},{"key":"21024_CR47","doi-asserted-by":"publisher","first-page":"104748","DOI":"10.1016\/j.bioorg.2021.104748","volume":"110","author":"WM Eldehna","year":"2021","unstructured":"Eldehna, W. M. et al. Development of isatin-thiazolo [3, 2-a] benzimidazole hybrids as novel CDK2 inhibitors with potent in vitro apoptotic anti-proliferative activity: Synthesis, biological and molecular dynamics investigations. Bioorg. Chem. 110, 104748 (2021).","journal-title":"Bioorg. Chem."},{"key":"21024_CR48","doi-asserted-by":"publisher","first-page":"99","DOI":"10.1016\/j.jim.2015.04.025","volume":"423","author":"S Pietkiewicz","year":"2015","unstructured":"Pietkiewicz, S., Schmidt, J. H. & Lavrik, I. N. Quantification of apoptosis and necroptosis at the single cell level by a combination of Imaging Flow Cytometry with classical Annexin V\/propidium iodide staining. J. Immunol. Methods 423, 99\u2013103 (2015).","journal-title":"J. Immunol. Methods"},{"key":"21024_CR49","doi-asserted-by":"publisher","first-page":"99","DOI":"10.1038\/sj.cdd.4400476","volume":"6","author":"AG Porter","year":"1999","unstructured":"Porter, A. G. & J\u00e4nicke, R. U. Emerging roles of caspase-3 in apoptosis. Cell Death Differ. 6, 99\u2013104 (1999).","journal-title":"Cell Death Differ."},{"key":"21024_CR50","doi-asserted-by":"publisher","first-page":"396","DOI":"10.1002\/prca.201400118","volume":"9","author":"TA Gorr","year":"2015","unstructured":"Gorr, T. A. & Vogel, J. Western blotting revisited: critical perusal of underappreciated technical issues. Proteom. Clin. Appl. 9, 396\u2013405 (2015).","journal-title":"Proteom. Clin. Appl."},{"key":"21024_CR51","doi-asserted-by":"publisher","first-page":"303","DOI":"10.1016\/j.acthis.2018.03.007","volume":"120","author":"E Grela","year":"2018","unstructured":"Grela, E., Koz\u0142owska, J. & Grabowiecka, A. Current methodology of MTT assay in bacteria\u2014A review. Acta Histochem. 120, 303\u2013311 (2018).","journal-title":"Acta Histochem."},{"key":"21024_CR52","unstructured":"Molecular Operating Environment (MOE), C. C. G. U., 1010 Sherbooke St. West, Suite #910, Montreal, QC, Canada, H3A 2R7, 2022."},{"key":"21024_CR53","doi-asserted-by":"publisher","first-page":"16233","DOI":"10.1073\/pnas.0908301106","volume":"106","author":"V Alterio","year":"2009","unstructured":"Alterio, V. et al. Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX. Proc. Natl. Acad. Sci. 106, 16233\u201316238 (2009).","journal-title":"Proc. Natl. Acad. Sci."},{"key":"21024_CR54","doi-asserted-by":"publisher","first-page":"825","DOI":"10.2174\/156802607780636690","volume":"7","author":"CT Supuran","year":"2007","unstructured":"Supuran, C. T. Carbonic anhydrases as drug targets-an overview. Curr. Top. Med. Chem. 7, 825\u2013833 (2007).","journal-title":"Curr. Top. Med. Chem."},{"key":"21024_CR55","doi-asserted-by":"publisher","first-page":"2210","DOI":"10.1016\/j.bmc.2017.02.037","volume":"25","author":"M Fares","year":"2017","unstructured":"Fares, M. et al. Synthesis of bulky-tailed sulfonamides incorporating pyrido [2, 3-d][1, 2, 4] triazolo [4, 3-a] pyrimidin-1 (5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects. Bioorg. Med. Chem. 25, 2210\u20132217 (2017).","journal-title":"Bioorg. Med. Chem."},{"key":"21024_CR56","doi-asserted-by":"publisher","first-page":"425","DOI":"10.1016\/j.bioorg.2018.09.007","volume":"81","author":"WM Eldehna","year":"2018","unstructured":"Eldehna, W. M. et al. Tumor-associated carbonic anhydrase isoform IX and XII inhibitory properties of certain isatin-bearing sulfonamides endowed with in vitro antitumor activity towards colon cancer. Bioorg. Chem. 81, 425\u2013432 (2018).","journal-title":"Bioorg. Chem."},{"key":"21024_CR57","doi-asserted-by":"publisher","first-page":"9004","DOI":"10.1021\/acs.jmedchem.5b01343","volume":"58","author":"J Leitans","year":"2015","unstructured":"Leitans, J. et al. Efficient expression and crystallization system of cancer-associated carbonic anhydrase isoform IX. J. Med. Chem. 58, 9004\u20139009 (2015).","journal-title":"J. Med. Chem."},{"key":"21024_CR58","volume-title":"Anticancer Drug Development Guide: Preclinical Screening, Clinical Trials, and Approval","author":"BA Teicher","year":"2013","unstructured":"Teicher, B. A. Anticancer Drug Development Guide: Preclinical Screening, Clinical Trials, and Approval (Springer, 2013)."},{"key":"21024_CR59","doi-asserted-by":"publisher","first-page":"838","DOI":"10.3390\/ijms19030838","volume":"19","author":"K Tatiparti","year":"2018","unstructured":"Tatiparti, K., Sau, S., Gawde, K. A. & Iyer, A. K. Copper-free \u2018click\u2019chemistry-based synthesis and characterization of carbonic anhydrase-IX anchored albumin-paclitaxel nanoparticles for targeting tumor hypoxia. Int. J. Mol. Sci. 19, 838 (2018).","journal-title":"Int. J. Mol. Sci."},{"key":"21024_CR60","doi-asserted-by":"publisher","first-page":"5701","DOI":"10.1016\/j.bmc.2010.06.009","volume":"18","author":"AA Sagardoy","year":"2010","unstructured":"Sagardoy, A. A. et al. Benzo [b] thiophene-6-carboxamide 1, 1-dioxides: Inhibitors of human cancer cell growth at nanomolar concentrations. Bioorg. Med. Chem. 18, 5701\u20135707 (2010).","journal-title":"Bioorg. Med. Chem."},{"key":"21024_CR61","doi-asserted-by":"publisher","first-page":"686","DOI":"10.1080\/14756366.2017.1421181","volume":"33","author":"WM Eldehna","year":"2018","unstructured":"Eldehna, W. M. et al. Novel [(3-indolylmethylene) hydrazono] indolin-2-ones as apoptotic anti-proliferative agents: design, synthesis and in vitro biological evaluation. J. Enzyme Inhib. Med. Chem. 33, 686\u2013700 (2018).","journal-title":"J. Enzyme Inhib. Med. Chem."},{"key":"21024_CR62","doi-asserted-by":"publisher","first-page":"600","DOI":"10.1080\/14756366.2017.1279155","volume":"32","author":"WM Eldehna","year":"2017","unstructured":"Eldehna, W. M. et al. Synthesis and in vitro anti-proliferative activity of some novel isatins conjugated with quinazoline\/phthalazine hydrazines against triple-negative breast cancer MDA-MB-231 cells as apoptosis-inducing agents. J. Enzyme Inhib. Med. Chem. 32, 600\u2013613 (2017).","journal-title":"J. Enzyme Inhib. Med. Chem."},{"key":"21024_CR63","doi-asserted-by":"publisher","first-page":"1095","DOI":"10.1080\/14756366.2018.1477137","volume":"33","author":"A Sabt","year":"2018","unstructured":"Sabt, A. et al. Novel coumarin-6-sulfonamides as apoptotic anti-proliferative agents: synthesis, in vitro biological evaluation, and QSAR studies. J. Enzyme Inhib. Med. Chem. 33, 1095\u20131107 (2018).","journal-title":"J. Enzyme Inhib. Med. Chem."},{"key":"21024_CR64","doi-asserted-by":"publisher","first-page":"290","DOI":"10.1016\/j.bioorg.2018.03.027","volume":"78","author":"HI Gul","year":"2018","unstructured":"Gul, H. I. et al. Anticancer effects of new dibenzenesulfonamides by inducing apoptosis and autophagy pathways and their carbonic anhydrase inhibitory effects on hCA I, hCA II, hCA IX, hCA XII isoenzymes. Bioorg. Chem. 78, 290\u2013297 (2018).","journal-title":"Bioorg. Chem."}],"container-title":["Scientific Reports"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.nature.com\/articles\/s41598-022-21024-7.pdf","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/www.nature.com\/articles\/s41598-022-21024-7","content-type":"text\/html","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/www.nature.com\/articles\/s41598-022-21024-7.pdf","content-type":"application\/pdf","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2022,10,6]],"date-time":"2022-10-06T12:23:21Z","timestamp":1665059001000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.nature.com\/articles\/s41598-022-21024-7"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2022,10,6]]},"references-count":64,"journal-issue":{"issue":"1","published-online":{"date-parts":[[2022,12]]}},"alternative-id":["21024"],"URL":"https:\/\/doi.org\/10.1038\/s41598-022-21024-7","relation":{},"ISSN":["2045-2322"],"issn-type":[{"value":"2045-2322","type":"electronic"}],"subject":[],"published":{"date-parts":[[2022,10,6]]},"assertion":[{"value":"19 June 2022","order":1,"name":"received","label":"Received","group":{"name":"ArticleHistory","label":"Article History"}},{"value":"21 September 2022","order":2,"name":"accepted","label":"Accepted","group":{"name":"ArticleHistory","label":"Article History"}},{"value":"6 October 2022","order":3,"name":"first_online","label":"First Online","group":{"name":"ArticleHistory","label":"Article History"}},{"value":"The authors declare no competing interests.","order":1,"name":"Ethics","group":{"name":"EthicsHeading","label":"Competing interests"}}],"article-number":"16756"}}