{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,15]],"date-time":"2026-08-15T01:36:44Z","timestamp":1786757804018,"version":"build-2736575974"},"reference-count":51,"publisher":"Wiley","issue":"12","license":[{"start":{"date-parts":[[2022,11,17]],"date-time":"2022-11-17T00:00:00Z","timestamp":1668643200000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Chemistry &amp; Biodiversity"],"published-print":{"date-parts":[[2022,12]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>The inhibition of phosphatidylinositol\u20104,5\u2010bisphosphate 3\u2010kinase catalytic subunit alpha (PIK3CA) protein could be a promising treatment for breast cancer. In this regard, docking studies were accomplished on various functionalized organic molecules. Among them, several derivatives of quinazolin\u20104(1<jats:italic>H<\/jats:italic>)\u2010one exhibited anti\u2010breast cancer activity and satisfied the drug likeliness properties. Further, the<jats:italic>in\u2005vitro<\/jats:italic>inhibitory studies by a series of 2\u2010(2\u2010phenoxyquinolin\u20103\u2010yl)\u20102,3\u2010dihydroquinazolin\u20104(1<jats:italic>H<\/jats:italic>)\u2010one molecules showed strong anti\u2010cancer activity than the currently available drug, wortmannin. The MTT cytotoxicity assay was used to predict the anti\u2010proliferative activity of these drugs against MCF\u20107 cancer cells by inhibiting the PIK3CA protein. The dose\u2010dependent analysis showed a striking decrease in cancer cell viability at 24 h with inhibitory concentrations (IC<jats:sub>50<\/jats:sub>) of<jats:bold>3b<\/jats:bold>,<jats:bold>3c<\/jats:bold>,<jats:bold>3d<\/jats:bold>,<jats:bold>3f<\/jats:bold>and<jats:bold>3m<\/jats:bold>are 15\u00b11, 17\u00b11, 8\u00b11, 10\u00b11 and 60\u00b11 (nanomoles), respectively. This is the first report in the literature on the inhibition of PIK3CA protein by quinazolinone derivatives that can be used in the treatment of cancer. Quinazolinone analogs have the potential to be safe and economically feasible scaffolds if they are produced using a chemical technique that is both straightforward and amenable to modification. From the cancer research perspective, this study can eventually offer better care for cancer patients.<\/jats:p>","DOI":"10.1002\/cbdv.202200662","type":"journal-article","created":{"date-parts":[[2022,10,20]],"date-time":"2022-10-20T02:20:28Z","timestamp":1666232428000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":8,"title":["Designing, Synthesis, and Anti\u2010Breast Cancer Activity of a Series of New Quinazolin\u20104(1<i>H<\/i>)\u2010one Derivatives"],"prefix":"10.1002","volume":"19","author":[{"given":"Manne","family":"Madhava Reddy","sequence":"first","affiliation":[{"name":"Department of Chemistry School of Advanced Sciences Vellore Institute of Technology Vellore 632014, Tamil Nadu India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rajagopal","family":"Desikan","sequence":"additional","affiliation":[{"name":"Department of Chemistry School of Advanced Sciences Vellore Institute of Technology Vellore 632014, Tamil Nadu India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sanjay","family":"Naik","sequence":"additional","affiliation":[{"name":"Center for Bioseparation Technology Vellore Institute of Technology Vellore 632014, Tamil Nadu India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sanjit","family":"Kumar","sequence":"additional","affiliation":[{"name":"Center for Bioseparation Technology Vellore Institute of Technology Vellore 632014, Tamil Nadu India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Thirumal","family":"Kumar D","sequence":"additional","affiliation":[{"name":"Department of Integrative Biology School of Biosciences and Technology Vellore Institute of Technology Vellore 632014, Tamil Nadu India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"George","family":"Priya Doss C","sequence":"additional","affiliation":[{"name":"Department of Integrative Biology School of Biosciences and Technology Vellore Institute of Technology Vellore 632014, Tamil Nadu India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5208-6307","authenticated-orcid":false,"given":"Akella","family":"Sivaramakrishna","sequence":"additional","affiliation":[{"name":"Department of Chemistry School of Advanced Sciences Vellore Institute of Technology Vellore 632014, Tamil Nadu India"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2022,11,17]]},"reference":[{"key":"e_1_2_9_1_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41392-021-00572-w"},{"key":"e_1_2_9_2_1","doi-asserted-by":"publisher","DOI":"10.1111\/cbdd.13860"},{"key":"e_1_2_9_3_1","first-page":"635","article-title":"\u2018Chemistry and pharmacological evaluation of quinazoline and quinazoline derivatives \u2013 a review\u2019","volume":"10","author":"John M. 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