Synthesis and biological evaluation of 2,5-diaminobenzamide derivatives as anti-proliferating agents.
The screening of the chemical library for the anti-proliferative activity of the chemical library provided 2,5-diaminobenzamide as the initial hit. The confirmation and the optimization of hit were performed by synthesis followed by the evaluation of growth inhibitory activity against human cancer cell lines. The most active growth inhibitor showed IC(50) of 1.0 microM. The compound 7 increased not only sub-G1 population but also number of cells which are stained with Annexin V-FITC and 7-AAD, suggesting that compound 7 induced cell death is apoptosis.
Lee
Sang-Hyo
SH
Department of Chemistry, Keimyung University, Daegu 704-701, Korea.
Park
Jong-Won
JW
Hong
Ji-Eun
JE
Park
Jong-Wook
JW
Lee
Jinho
J
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D017209:Apoptosis; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D054852:Small Molecule Libraries / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D001549:Benzamides; D054852:Small Molecule Libraries