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

Document Type : Research article

Authors

1 Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

2 Protein Technology Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

3 Department of Toxicology and Pharmacology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

10.22037/ijpr.2021.114865.15076

Abstract

Cancers 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.

Graphical Abstract

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

Keywords


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