期刊
BIOORGANIC CHEMISTRY
卷 77, 期 -, 页码 515-526出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2018.02.005
关键词
Imidazo[2,1-b]thiazoles; Benzimidazole; Cytotoxicity; Cell cycle; Apoptosis
资金
- CSIR - India
- UGC, New Delhi, India
- project 'Affordable Cancer Therapeutics (ACT)' under XIIth five-year plan
A series of imidazo[2,1-b]thiazole-benzimidazole conjugates were synthesized and evaluated for their antiproliferative activity against four human cancer cell lines i.e.; HeLa (cervical), A549 (lung), MCF-7 (breast) and DU-145 (prostate) along with normal HEK-293 cell line. Amongst them, conjugate 6d displayed significant cytotoxicity against human lung cancer cell line, A549 with IC50 value 1.08 mu M Further, cell cycle analysis revealed that this compound arrested the cell cycle at G2/M phase in A549 cells. Furthermore, the tubulin polymerization assay results suggest that this conjugate (6d) exhibits significant inhibitory effect on the tubulin assembly with an IC50 value of 1.68 mu M. Moreover, the apoptotic inducing properties of compound 6d was confirmed by Hoechst staining, measurement of mitochondrial membrane potential (Delta Psi m)and annexin V-FITC assay. Further, molecular docking studies revealed that compound 6d occupied the colchicine binding site. (C) 2018 Elsevier Inc. All rights reserved.
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