Research Article | Volume: 7, Issue: 3, March, 2017

Novel Thiadiazole Derivatives as Bcr-Abl Tyrosine Kinase Inhibitors

Vijayakumar Subramanian Sulaiman Ali Muhammad Kaveri Sundaram Subban Ravi   

Open Access   

Published:  Mar 30, 2017

DOI: 10.7324/JAPS.2017.70311
Abstract

The present work mainly aims to discover novel small molecular inhibitors against important molecular target T3151 Abl mutant involved in leukemia. Five heterocyclic compounds 1-5 with N and S atoms (thiosemicarbazone, thiadiazole and thiazolidinoyl derivatives) were synthesised and characterised using spectral data. Docking study was carried out for 1-5 against the T315I Bcr-Abl mutant. The compounds 3-5 with phenothiazine pharmacophore showed promising docking score than with the derivatives having the coumarin pharmacophore 1 and 2. So the compounds 3-5 were tested for their anticancer activity against leukemic K562 cell line by trypan blue, MTT and LDH assays. Compound 5 showed marked anticancer activity and exhibited an IC50 value of 11.12 and 50.66 µg/ml against trypan blue and MTT assay respectively. Further a dose-dependent increase in LDH release was observed, confirming the antiproliferative potential of the compounds.


Keyword:     Chronic myelogenous leukemia thiadiazole synthesis characterisation molecular docking antiproliferative activity.


Citation:

Subramanian V, Muhammad SA, Sundaram K, Ravi S. Novel Thiadiazole Derivatives as Bcr-Abl Tyrosine Kinase Inhibitors. J App Pharm Sci, 2017; 7 (03): 068-076.

Copyright:The Author(s). This is an open access article distributed under the Creative Commons Attribution Non-Commercial License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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