Journal
JOURNAL OF TAIBAH UNIVERSITY FOR SCIENCE
Volume 12, Issue 4, Pages 382-392Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/16583655.2018.1489036
Keywords
Thiadiazolopyrimidinone; anticancer activity; bovine serum albumin; molecular docking
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Funding
- Department of Science & Technology (DST-SERB), Govt. of India, New Delhi [SR/S1/OC-58/2011]
- University Grant Commission (UGC), NewDelhi under UPE-FAR-I program [14-3/2012(NS/PE)]
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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.
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