Synthesis and In Vitro Antiproliferative Activity of Diphenyl(piperidin-4-yl) thioamide Methanol Derivatives

doi:10.2174/157018008785909804

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Synthesis and In Vitro Antiproliferative Activity of Diphenyl(piperidin-4-yl) thioamide Methanol Derivatives

Published Oct 1, 2008 · S. Prasad, M. Vinaya, C. S. A. Kumar

Letters in Drug Design & Discovery

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Abstract

A series of novel diphenyl(piperidin-4-yl) methanol derivatives 10(a-j) were synthesized and characterized by H-1 NMR, LC/MS, FTIR and elemental analyses. All the compounds synthesised were evaluated for their cell antiproliferation activity by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. The antiproliferative effects of the synthesised compounds were tested against viable human skin fibroblast cell line and carcinoma cell lines namely HeLa, HT-29, MCF-7, HepG-2 by adopting positive and negative control. The importance of the methoxy and fluorine group on diphenyl(piperidin-4-yl) methanol moiety was confirmed and it was noted that, the substitution at 4(th) position of the aryl ring plays a dominant role and was responsible for the antiproliferative activity. Among the synthesized compounds, only (10a) and (10b) have potent antiproliferative activity on all the carcinoma cell lines tested.

In Vitro Study

Study Snapshot

Diphenyl(piperidin-4-yl) thioamide methanol derivatives 10a and 10b show potent antiproliferative activity against various carcinoma cell lines, with the substitution at the 4th position of the aryl ring playing a dominant role.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Synthesis and In Vitro Antiproliferative Activity of Diphenyl(piperidin-4-yl) thioamide Methanol Derivatives

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