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chlorides 6a-b. Five new series of chalcone-sulfonamide hybrids (16-20)a-f were prepared via Claisen\u2013Schmidt condensation of the newly obtained sulfonamides with aromatic aldehydes 15a-f in basic medium. Chalcones substituted with chlorine at position 4 of each series were used as precursors for the generation of their five-membered heterocyclic pyrazoline (22-23)a-d, (24-25)a-b and carbothioamide 27a-f derivatives. The synthesized compounds were evaluated for their anticancer and antituberculosis activities. To determine their anticancer activity, compounds were screened against sixty human cancer cell lines at a single dose (10 \u03bcM). Compounds 17a-c were highly active against LOX IMVI (melanoma), with IC50 values of 0.34, 0.73 and 0.54 \u03bcM, respectively. Chalcone 18e showed remarkable results against the entire panel of leukemia cell lines with IC50 values between 0.99\u20132.52 \u03bcM. Moreover, compounds 20e and 20f displayed growth inhibition of Mycobacterium tuberculosis H37Rv at concentrations below 10 \u03bcM. Although they showed low selectivity in cytotoxicity tests against the Vero cell line, further optimization could advance the potential biological activity of the selected compounds.<\/jats:p>","DOI":"10.3390\/ijms232012589","type":"journal-article","created":{"date-parts":[[2022,10,20]],"date-time":"2022-10-20T22:49:46Z","timestamp":1666306186000},"page":"12589","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":26,"title":["Synthesis, Anticancer and Antitubercular Properties of New Chalcones and Their Nitrogen-Containing Five-Membered Heterocyclic Hybrids Bearing Sulfonamide Moiety"],"prefix":"10.3390","volume":"23","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-0503-1944","authenticated-orcid":false,"given":"Lina Fernanda","family":"Casta\u00f1o","sequence":"first","affiliation":[{"name":"Heterocyclic Compounds Research Group, Department of Chemistry, Universidad del Valle, A.A., Cali 25360, Colombia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9451-3063","authenticated-orcid":false,"given":"Jairo","family":"Quiroga","sequence":"additional","affiliation":[{"name":"Heterocyclic Compounds Research Group, Department of Chemistry, Universidad del Valle, A.A., Cali 25360, Colombia"},{"name":"Centre for Bioinformatics and Photonics-CIBioFI, Universidad del Valle, A.A., Cali 25360, Colombia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3256-0961","authenticated-orcid":false,"given":"Rodrigo","family":"Abonia","sequence":"additional","affiliation":[{"name":"Heterocyclic Compounds Research Group, Department of Chemistry, Universidad del Valle, A.A., Cali 25360, Colombia"},{"name":"Centre for Bioinformatics and Photonics-CIBioFI, Universidad del Valle, A.A., Cali 25360, Colombia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9662-9505","authenticated-orcid":false,"given":"Daniel","family":"Insuasty","sequence":"additional","affiliation":[{"name":"Department of Chemistry and Biology, Basic Sciences Division, Universidad del Norte, Barranquilla 081007, Colombia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7807-1242","authenticated-orcid":false,"given":"Oscar M.","family":"Vidal","sequence":"additional","affiliation":[{"name":"Department of Medicine, Health Division, Universidad del Norte, Barranquilla 081007, Colombia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5677-2614","authenticated-orcid":false,"given":"Rosalia","family":"Se\u00f1a","sequence":"additional","affiliation":[{"name":"Department of Chemistry and Biology, Basic Sciences Division, Universidad del Norte, Barranquilla 081007, Colombia"},{"name":"Department of Medicine, Health Division, Universidad del Norte, Barranquilla 081007, Colombia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Vivian","family":"Rubio","sequence":"additional","affiliation":[{"name":"Grupo de Micobacterias, Red TB. Direcci\u00f3n de Investigaci\u00f3n en Salud P\u00fablica, Instituto Nacional de Salud, Bogot\u00e1 111321, Colombia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gloria","family":"Puerto","sequence":"additional","affiliation":[{"name":"Grupo de Micobacterias, Red TB. Direcci\u00f3n de Investigaci\u00f3n en Salud P\u00fablica, Instituto Nacional de Salud, Bogot\u00e1 111321, Colombia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5976-0387","authenticated-orcid":false,"given":"Manuel","family":"Nogueras","sequence":"additional","affiliation":[{"name":"Department of Inorganic and Organic Chemistry, Universidad de Ja\u00e9n, 23071 Ja\u00e9n, Spain"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9184-2390","authenticated-orcid":false,"given":"Justo","family":"Cobo","sequence":"additional","affiliation":[{"name":"Department of Inorganic and Organic Chemistry, Universidad de Ja\u00e9n, 23071 Ja\u00e9n, Spain"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4120-9065","authenticated-orcid":false,"given":"Juan","family":"Guzman","sequence":"additional","affiliation":[{"name":"Department of Bioresources, Fraunhofer Institute for Molecular Biology and Applied Ecology, 35392 Giessen, Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alberto","family":"Insuasty","sequence":"additional","affiliation":[{"name":"Nanostructured Functional Materials Research Group, Universidad CESMAG, Pasto 520003, Colombia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8371-3310","authenticated-orcid":false,"given":"Braulio","family":"Insuasty","sequence":"additional","affiliation":[{"name":"Heterocyclic Compounds Research Group, Department of Chemistry, Universidad del Valle, A.A., Cali 25360, Colombia"},{"name":"Centre for Bioinformatics and Photonics-CIBioFI, Universidad del Valle, A.A., Cali 25360, Colombia"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2022,10,20]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"367","DOI":"10.1097\/CEJ.0000000000000594","article-title":"Progress in Cancer Mortality, Incidence, and Survival: A Global Overview","volume":"29","author":"Santucci","year":"2020","journal-title":"Eur. 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