Premium
Synthesis and Biological Evaluation of Thieno[2, 3‐ d ]pyrimidine‐amides as Potential Anticancer Agents
Author(s) -
Ramya Posa Venkata Sri,
Thatikonda Sowjanya,
Angapelly Srinivas,
Babu Bathini Nagendra,
Naidu Vegi Ganga Modi,
Kamal Ahmed
Publication year - 2018
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201703061
Subject(s) - clonogenic assay , dapi , apoptosis , flow cytometry , cell cycle , growth inhibition , cell culture , pyrimidine , cell growth , cell cycle checkpoint , chemistry , stereochemistry , microbiology and biotechnology , biology , cancer research , biochemistry , genetics
In our search towards the development of potential anticancer agents, a new class of N ‐(3‐(thieno[2, 3‐ d ]pyrimidin‐4‐ylamino)phenyl)amides ( 10 a−x ) were synthesized and examined for their anticancer activity towards different human cancer cell lines. Of the derivatives tested, 10 g , 10 p and 10 w displayed potent growth inhibition on some of the cell lines, peculiarly 10 w exhibited selective and promising activity on MDA‐MB‐453 and MCF‐7 cell lines. In comparison to the standard ZSTK474, nearly 3 fold growth inhibitory effect was noticed with 10 w against MCF‐7 cell line. Notably, the morphology and long term clonogenic survival of MCF‐7 cells were affected by compound 10 w . Moreover, the results from AO/EB and DAPI staining studies as well as analysis of mitochondrial membrane potential divulged that the growth of MCF‐7 cells was inhibited by 10 w through the induction of apoptosis. From flow‐cytometry analysis, it is notable that 10 w shows G0/G1 cell cycle arrest in MCF‐7 cells. Overall, compound 10 w could be considered as a promising lead for the further exploration and identification of thieno[2, 3‐ d ]pyrimidine‐based anticancer agents.