Design and synthesis of novel N-[3-(benzimidazol-2-ylamino)phenyl]amine and N-[3-(benzoxazol-2-ylamino)phenyl]amine derivatives as potential anticancer agents

• Published in: Molecular diversity Vol. 26; no. 4; pp. 2269 - 2293
• Main Authors: Kumar, Honnavalli Yogish, Murumkar, Prashant R., Srinivasan, B. P., Pawar, Vijay, Yadav, M. R.
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01.08.2022; Springer Nature B.V
• Subjects: Biochemistry; Biomedical and Life Sciences; Breast cancer; Cell cycle; Chemists; Clinical trials; Cytotoxicity; Design; Flow cytometry; Kinases; Leukemia; Life Sciences; Organic Chemistry; Original Article; Pharmaceuticals; Pharmacy; Polymer Sciences; Flow cytometry; Cytotoxicity; National Cancer Institute; Anticancer agents; [3-(benzimidazol-2-yl-amino)phenyl]amine
• ISSN: 1381-1991; 1573-501X
• DOI: 10.1007/s11030-021-10333-0

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 µM” and “0.276–12.3 µM,” 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.