Discovery of Pyrrole−Indoline-2-ones as Aurora Kinase Inhibitors with a Different Inhibition Profile

A series of pyrrole−indolin-2-ones were synthesized, and their inhibition profile for Aurora kinases was studied. The potent compound 33 with phenylsulfonamido at the C-5 position and a carboxyethyl group at the C-3′ position selectively inhibited Aurora A over Aurora B with IC50 values of 12 and 15...

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Veröffentlicht in:	Journal of medicinal chemistry 2010-08, Vol.53 (16), p.5929-5941
Hauptverfasser:	Chiang, Chao-Cheng, Lin, Yu-Hsiang, Lin, Shu Fu, Lai, Chun-Liang, Liu, Chiawei, Wei, Win-Yin, Yang, Sheng-chuan, Wang, Ru-Wen, Teng, Li-Wei, Chuang, Shih-Hsien, Chang, Jia-Ming, Yuan, Ta-Tung, Lee, Ying-Shuen, Chen, Paonien, Chi, Wei-Kuang, Yang, Ju-Ying, Huang, Hung-Jyun, Liao, Chu-Bin, Huang, Jiann-Jyh
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Aurora Kinase B Aurora Kinases Cell Proliferation - drug effects Drug Screening Assays, Antitumor HCT116 Cells HeLa Cells Histones - metabolism HT29 Cells Humans Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Models, Molecular Phosphorylation Protein Binding Protein-Serine-Threonine Kinases - antagonists & inhibitors Pyrroles - chemical synthesis Pyrroles - chemistry Pyrroles - pharmacology Stereoisomerism Structure-Activity Relationship
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