204841-35-0Relevant articles and documents
Antitumor agents. Part 202: Novel 2'-amino chalcones: Design, synthesis and biological evaluation
Xia, Yi,Yang, Zheng-Yu,Xia, Peng,Bastow, Kenneth F.,Nakanishi, Yuka,Lee, Kuo-Hsiung
, p. 699 - 701 (2007/10/03)
New 4',5',2,3,4-substituted 2'-amino chalcones were synthesized and evaluated for cytotoxicity against a panel of human tumor cell lines. Several compounds displayed significant cytotoxicity. The most promising lead molecule (10) also had high activity to
Antitumor agents. 181. Synthesis and biological evaluation of 6,7,2',3',4'-substituted-1,2,3,4-tetrahydro-2-phenyl-4-quinolones as a new class of antimitotic antitumor agents
Xia, Yi,Yang, Zheng-Yu,Xia, Peng,Bastow, Kenneth F.,Tachibana, Yoko,Kuo, Sheng-Chu,Hamel, Ernest,Hackl, Torben,Lee, Kuo-Hsiung
, p. 1155 - 1162 (2007/10/03)
A novel series of 6,7,2',3',4'-substituted-1,2,3,4-tetrahydro-2-phenyl- 4-quinolones were synthesized and evaluated for interactions with tubulin and for cytotoxic activity against a panel of human tumor cell lines, including ileocecal carcinoma (HCT-8), breast cancer (MCF-7), lung carcinoma (A-549), epidermoid carcinoma of the nasopharynx (KB), renal cancer (CAKI-1), and melanoma cancer (SKMEL-2). Most compounds (18, 20, 22-27) showed potent cytotoxic and antitubulin effects. The most active compounds (23, 26, 27) demonstrated strong cytotoxic effects with ED50 values in the nanomolar or subnanomolar range in almost all tumor cell lines. Three active racemates (20, 22, 25) were separated into the enantiomers, and generally, the optically pure (-)-isomers (20a, 22a, 25a) exhibited greater biological activity than the racemates or (+)-isomers. Cytotoxicity and antitubulin activity were closely correlated, with the most active compounds (23, 26, 27) having effects comparable to those of colchicine, podophyllotoxin, and combretastatin A-4.