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

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

Volume: 5 Issue: 7

Author(s): Salekoppal Boregowda Benaka Prasad, Mallappanahally Kambappa Vinaya, Channapille Koppal Siddegowda Ananda Kumar, Sanjay Swarup and Kanchugarakoppal Subbegowda Rangappa

Affiliation:

Keywords: Diphenyl(pyridin-4-yl)methanol, Isothiocyanates, MTT assay, Antiproliferative activity, Cancer therapy, Cell proliferation

Abstract: A series of novel diphenyl(piperidin-4-yl)methanol derivatives 10(a-j) were synthesized and characterized by 1H 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 4th 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.

Cite this article as:

Benaka Prasad Boregowda Salekoppal, Vinaya Kambappa Mallappanahally, Ananda Kumar Koppal Siddegowda Channapille, Swarup Sanjay and Rangappa Subbegowda Kanchugarakoppal, Synthesis and In Vitro Antiproliferative Activity of Diphenyl(piperidin-4- yl)thioamide Methanol Derivatives, Letters in Drug Design & Discovery 2008; 5 (7) . https://dx.doi.org/10.2174/157018008785909804