Journal
MOLECULAR DIVERSITY
Volume 26, Issue 4, Pages 2269-2293Publisher
SPRINGER
DOI: 10.1007/s11030-021-10333-0
Keywords
N-[3-(benzimidazol-2-yl-amino)phenyl]amine; Flow cytometry; Cytotoxicity; National Cancer Institute; Anticancer agents
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Funding
- NCT Delhi Government
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This study reported the design, synthesis, and cytotoxicity studies of a series of derivatives, with two compounds showing remarkable cytotoxicity and inducing cell cycle arrest and apoptosis in leukemia cancer cells.
In this contribution, we report the design, synthesis and cytotoxicity studies of a series of N-[3-(benzimidazol-2-yl-amino)phenyl]amine and N-[3-(benzoxazol-2-ylamino)phenyl]amine derivatives. In vitro cytotoxicity assay of 26 selected compounds was carried out at National Cancer Institute (NCI), USA. Out of them, compounds 10e (NSC D-762842/1) and 11s (NSC D-764942/1) have shown remarkable cytotoxicity with GI(50) values ranging between 0.589-14.3 mu M and 0.276-12.3 mu M, respectively, in the representative nine subpanels of human tumor cell lines. Further, flow cytometry analysis demonstrated that compound 10e exerted cell cycle arrest at G2/M phase and showed dose-dependent enhancement in apoptosis in K-562 leukemia cancer cells.
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