1. Synthesis and biological evaluation of novel pyrimidine-benzimidazol hybrids as potential anticancer agents.
- Author
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Shao KP, Zhang XY, Chen PJ, Xue DQ, He P, Ma LY, Zheng JX, Zhang QR, and Liu HM
- Subjects
- Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Benzimidazoles chemistry, Cell Cycle drug effects, Cell Death drug effects, Cell Line, Tumor, Cell Proliferation drug effects, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Humans, MCF-7 Cells, Molecular Structure, Pyrimidines chemistry, Structure-Activity Relationship, Antineoplastic Agents pharmacology, Benzimidazoles pharmacology, Pyrimidines pharmacology
- Abstract
A series of pyrimidine-benzimidazol hybrids was synthesized and evaluated for anticancer activity on four human cancer cell lines including MCF-7, MGC-803, EC-9706 and SMMC-7721. Some of the synthesized compounds exhibited moderate to potent activity against MGC-803 and MCF-7. Among them, compounds 5a-b and 6a-b showed most effective activity. Compounds 5b and 6b were more cytotoxic than 5-fluorouracil against all tested four human cancer cell lines, with IC50 values ranging from 2.03 to 10.55 μM and 1.06 to 12.89 μM, respectively. Flow cytometry analysis demonstrated that treatment of MGC-803 with 6b led to cell cycle arrest at G2/M phase accompanied by an increase in apoptotic cell death., (Copyright © 2014. Published by Elsevier Ltd.)
- Published
- 2014
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