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Synthesis and in vitro anticancer activity of 6-chloro-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one derivatives: molecular docking and interaction with bovine serum albumin

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journal contribution
posted on 2018-06-25, 10:18 authored by Supreet Gaonkar, Manjunath G. Sunagar, Narahari Deshapande, Ningaraddi S. Belavagi, Shrinivas D Joshi, Sheshagiri R Dixit, Imtiyaz Ahmed M. Khazi

A novel series of 6-chloro-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one derivatives were synthesized. Structure of the newly synthesized compounds was established by their analytical and spectroscopic data. The title compounds were evaluated for their anticancer activity against human breast cancer (T-47D) and lung cancer (NCI-H226) cell lines. Effects of compounds on the cell morphology of these cell lines were studied. Among the series of compounds tested, 6-chloro-7-methyl-2-(4-((2-(piperidin-1-yl)ethylamino)methyl) phenyl)-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one [MTDP4(9)] exhibited good anticancer activity against both cell lines. Further, the binding interaction of [MTDP4(9)] with bovine serum albumin has been investigated by UV, fluorescence and molecular docking studies.

Funding

The authors gratefully acknowledge the financial assistance from Department of Science & Technology (DST-SERB), Govt. of India, New Delhi under Major Research Project No. SR/S1/OC-58/2011 and University Grant Commission (UGC), New Delhi under UPE-FAR-I program, F. No. 14-3/2012 (NS/PE).

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