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A virtual screening was conducted on a library consisting of 265,242 chemical compounds, with the objective of identifying molecules that exhibit structural similarities to the furan chalcone scaffold. Further, PHD\u20102 activation potential of screened compound was determined using in vitro 2\u2010oxoglutarate assay. The cytotoxic activity and apoptotic potential of screened compound was determined using various staining techniques, including 3\u2010(4,5\u2010dimethylthiazol\u20102\u2010yl)\u20102,5\u2010diphenyl tetrazolium bromide, 4\u2032,6\u2010diamidino\u20102\u2010phenylindole (DAPI), 1,1\u2032,3,3\u2032\u2010tetraethylbenzimi\u2010dazolylcarbocyanine iodide (JC\u20101), and acridine orange\/ethidium bromide (AO\/EB), against MCF\u20107 cells. 7,12\u2010Dimethylbenz[<jats:italic>a<\/jats:italic>]anthracene (DMBA) model of mammary gland cancer was used to study the in vivo antineoplastic efficacy of screened compound. [(<jats:italic>E<\/jats:italic>)\u20101\u2010(4\u2010fluorophenyl)\u20103\u2010(furan\u20102\u2010yl) prop\u20102\u2010en\u20101\u2010one] (BBAP\u20107) was screened and validated as a PHD\u20102 activator by an in vitro 2\u2010oxo\u2010glutarate assay. The IC<jats:sub>50<\/jats:sub> of BBAP\u20107 on MCF\u20107 cells is 18.84\u2009\u00b5M. AO\/EB and DAPI staining showed nuclear fragmentation, blebbing and condensation in MCF\u20107 cells following BBAP\u20107 treatment. The red\u2010to\u2010green intensity ratio of JC\u20101 stained MCF\u20107 cells decreased after BBAP\u20107 treatment, indicating mitochondrial\u2010mediated apoptosis. DMBA caused mammary gland dysplasia, duct hyperplasia and ductal carcinoma in situ. Carmine staining, histopathology, and scanning electron microscopy demonstrated that BBAP\u20107, alone or with tirapazamine, restored mammary gland surface morphology and structural integrity. Additionally, BBAP\u20107 therapy significantly reduced oxidative stress and glycolysis. The findings reveal that BBAP\u20107 activates PHD\u20102, making it a promising anticancer drug.<\/jats:p>","DOI":"10.1002\/jbt.23679","type":"journal-article","created":{"date-parts":[[2024,3,16]],"date-time":"2024-03-16T06:12:04Z","timestamp":1710569524000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":6,"title":["Novel furan chalcone modulates PHD\u20102 induction to impart antineoplastic effect in mammary gland carcinoma"],"prefix":"10.1002","volume":"38","author":[{"given":"Shubham","family":"Rastogi","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical Sciences, School of Biomedical and Pharmaceutical Sciences Babasaheb Bhimrao Ambedkar University (A Central University) Lucknow Uttar Pradesh India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Mohd Nazam","family":"Ansari","sequence":"additional","affiliation":[{"name":"Department of Pharmacology, College of Pharmacy Prince Sattam Bin Abdulaziz University Al\u2010Kharaj Saudi Arabia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Abdulaziz S.","family":"Saeedan","sequence":"additional","affiliation":[{"name":"Department of Pharmacology, College of Pharmacy Prince Sattam Bin Abdulaziz University Al\u2010Kharaj Saudi Arabia"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sunil Kumar","family":"Singh","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Sciences, United Institute of Pharmacy United Group of Institutions Prayagraj India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Alok","family":"Mukerjee","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Sciences, United Institute of Pharmacy United Group of Institutions Prayagraj India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1649-5434","authenticated-orcid":false,"given":"Gaurav","family":"Kaithwas","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Sciences, School of Biomedical and Pharmaceutical Sciences Babasaheb Bhimrao Ambedkar University (A Central University) Lucknow Uttar Pradesh India"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2024,3,14]]},"reference":[{"key":"e_1_2_11_2_1","doi-asserted-by":"publisher","DOI":"10.3322\/caac.21660"},{"key":"e_1_2_11_3_1","doi-asserted-by":"publisher","DOI":"10.1002\/ijc.33588"},{"key":"e_1_2_11_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.gendis.2018.05.001"},{"key":"e_1_2_11_5_1","doi-asserted-by":"publisher","DOI":"10.2147\/HP.S93413"},{"key":"e_1_2_11_6_1","doi-asserted-by":"publisher","DOI":"10.2147\/HP.S53576"},{"key":"e_1_2_11_7_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.lfs.2019.117167"},{"key":"e_1_2_11_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molmed.2018.10.006"},{"key":"e_1_2_11_9_1","doi-asserted-by":"publisher","DOI":"10.1038\/sj.bjc.6605682"},{"key":"e_1_2_11_10_1","doi-asserted-by":"crossref","first-page":"1","DOI":"10.3389\/fnins.2017.00239","volume":"11","author":"Badawi Y.","year":"2017","journal-title":"Front. 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