Design, Synthesis and Biological Evaluation of 1,3-Diphenyl-3-(phenylthio)propan-1-ones as New Cytotoxic Agents

AuthorMaryam Bayanatien
AuthorSoraya Shahhosseinien
AuthorFarshad. H. Shirazien
AuthorGolrokh Farnamen
AuthorAfshin Zarghien
Issued Date2021-10-31en
AbstractCancers in terms of morbidity and mortality are one of the major universal issues. New compounds of anticancer agents based on β-aryl-β-mercapto ketones scaffold possessing piperidinylethoxy or morpholinylethoxy groups were synthesized and evaluated as cytotoxic agents. Cytotoxic effects of synthesized compounds were measured against MCF-7, human ER-positive breast cancer cell lines, using MTT assay. The results indicated that all compounds had high cytotoxic activity on MCF-7 cancerous cells, even more than the reference drug Tamoxifen. Among them, compounds 3-(4-(2-morpholinoethoxy)phenyl)-1-phenyl-3-(phenylthio)propan-1-one (4a) and 1-(4-methoxyphenyl)-3-(3-(2-morpholinoethoxy)phenyl)-3-(phenylthio)propan-1-one (4h) had no significant cytotoxic effects on normal cells compared to Tamoxifen. Our results also indicated that adding tertiary amine basic side chain, found in Tamoxifen drug, to 1,3-diphenyl-3-(phenylthio)propan-1-ones improves the cytotoxic effects of these compounds on breast cancer cells.en
DOIhttps://doi.org/10.22037/ijpr.2021.114865.15076en
KeywordSynthesisen
Keyword1en
Keyword3-Diphenyl-3-(phenylthio)propan-1-oneen
KeywordDocking studyen
KeywordCytotoxic effecten
KeywordMTTen
KeywordMCF-7en
PublisherBrieflandsen
TitleDesign, Synthesis and Biological Evaluation of 1,3-Diphenyl-3-(phenylthio)propan-1-ones as New Cytotoxic Agentsen
TypeOriginal Articleen

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