Synthesis and cytotoxicity evaluation of novel indolylpyrimidines and indolylpyrazines as potential antitumor agents

Citation
B. Jiang et al., Synthesis and cytotoxicity evaluation of novel indolylpyrimidines and indolylpyrazines as potential antitumor agents, BIO MED CH, 9(5), 2001, pp. 1149-1154
Citations number
20
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
9
Issue
5
Year of publication
2001
Pages
1149 - 1154
Database
ISI
SICI code
0968-0896(200105)9:5<1149:SACEON>2.0.ZU;2-4
Abstract
Novel indolylpyrimidines and indolylpyrazines have been synthesized as pote ntial antitumor agents. They were screened in a panel of 60 human tumor cel l lines in vitro. Compounds 7, 9, 10, 15, 21 exhibited efficiently cytotoxi c activities with GI(50) values in the low micromolar range against a varie ty of human cancer cell lines. 2,4-Bis(3'-indolyl)pyrimidine 8 displayed se lective cytotoxic activity against IGROV1 tumor cell line with the GI(50) v alue below 0.01 muM. (C) 2001 Elsevier Science Ltd. All rights reserved.