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Design and synthesis of optically pure 3-aryl-6-methyl-2-thioxotetrahydropyrimidin-4(1H)-ones as anti-prostate cancer agents

Publication Type : Journal Article

Publisher : Royal Society of Chemistry

Source : RSC Advances, 2014

Campus : Amritapuri

School : School of Biotechnology

Verified : No

Year : 2014

Abstract : 3-Aryl-6-methyl-2-thioxotetrahydropyrimidin-4(1H)-ones were proposed as a new class of anti-prostate cancer agents on the basis of molecular modeling studies. Stereoselective synthesis of 3-aryl-6-methyl-2-thioxotetrahydropyrimidin-4(1H)-one derivatives was achieved by chiral induction employing (R)/(S)-α-methyl benzylamine and subsequent debenzylation with HBr in AcOH afforded the desired enantiomers in good yields. The compounds were screened in vitro against prostate cancer cell lines, PC-3 and LNCaP and the most potent derivatives were identified.

Cite this Research Publication : Varun Kumar, Mahesh Rachamalla, Prajwal Nandekar, Gopal L. Khatik, Abhay T. Sangamwar, Kulbhushan Tikoo and Vipin A. Nair "Design and synthesis of optically pure 3-aryl-6-methyl-2-thioxotetrahydropyrimidin-4(1H)-ones as anti-prostate cancer agents", RSC Advances 2014, 4, 37868-37877

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