Synthesis and biological evaluation of novel anthranilamide derivatives as anticancer agents.
A new series of anthranilamide derivatives were synthesized and evaluated for their antiproliferative activities against human colon carcinoma cell lines (HCT 116) and human breast adenocarcinoma cell lines (MDA-MB-231) in vitro. The bioassay results indicated that compounds 7a-7d, 11a, and 11b with flexible linkers showed promising antiproliferative activity against both cell lines. Among the compounds synthesized, 7c showed the most significant antiproliferative activity. Flow cytometric analysis indicated that 7c inhibited HCT 116 and MDA-MB-231 cell growth by inducing apoptosis in a dose-dependent manner and suppressed HCT 116 cell proliferation by G1 and S phase arrest. Compound 7c may serve as a lead candidate in the development of novel anticancer agents.
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Ji'nan, Shandong, China.
Jianzhen
J
Liu
Wen
W
Liang
Yuanyou
Y
Wang
Guisen
G
Zhao
D000230:Adenocarcinoma / Q000473:pathology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D017209:Apoptosis; D001943:Breast Neoplasms / Q000473:pathology; D049109:Cell Proliferation / Q000187:drug effects; D015179:Colorectal Neoplasms / Q000473:pathology; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005260:Female; D059585:G1 Phase Cell Cycle Checkpoints / Q000187:drug effects; D045325:HCT116 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D062367:ortho-Aminobenzoates / Q000138:chemical synthesis* / Q000494:pharmacology*
D000970:Antineoplastic Agents; D062367:ortho-Aminobenzoates; C000219:anthranilamide