Document Detail


Synthesis and antiproliferative activity of imidazo[2,1-b][1,3,4]thiadiazole derivatives.
MedLine Citation:
PMID:  25205189     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
A series of 2,5,6-substituted imidazo[2,1-b][1,3,4]thiadiazole derivatives have been prepared and were tested for antiproliferative activity on cancer cells at the National Cancer Institute. Results showed that molecules with a benzyl group at position 2, exhibited an increase in activity for the introduction of a formyl group at the 5 position. The compound 2-benzyl-5-formyl-6-(4-bromophenyl)imidazo[2,1-b][1,3,4]thiadiazole 22 has been chosen for understanding the mechanism of action by various molecular and cellular biology studies. Results obtained from cell cycle evaluation analysis, analysis of mitochondrial membrane potential and Annexin V-FITC by flow cytometric analysis, ROS production and expression of apoptotic and DNA-repair proteins suggested that compound 22 induced cytotoxicity by activating extrinsic pathway of apoptosis, however, without affecting cell cycle progression.
Authors:
Sujeet Kumar; Vidya Gopalakrishnan; Mahesh Hegde; Vivek Rana; Sharad S Dhepe; Sureshbabu A Ramareddy; Alberto Leoni; Alessandra Locatelli; Rita Morigi; Mirella Rambaldi; Mrinal Srivastava; Sathees C Raghavan; Subhas S Karki
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-8-26
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2014 Aug 
Date Detail:
Created Date:  2014-9-10     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2014 Elsevier Ltd. All rights reserved.
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