Synthesis and cytotoxicity evaluation of novel indolylpyrimidines and indolylpyrazines as potential antitumor agents.
Novel indolylpyrimidines and indolylpyrazines have been synthesized as potential antitumor agents. They were screened in a panel of 60 human tumor cell lines in vitro. Compounds 7, 9, 10, 15, 21 exhibited efficiently cytotoxic activities with GI(50) values in the low micromolar range against a variety of human cancer cell lines. 2,4-Bis(3'-indolyl)pyrimidine 8 displayed selective cytotoxic activity against IGROV1 tumor cell line with the GI(50) value below 0.01 microM.
Jiang
B
B
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, P. R., Shanghai 200032, China. jiangb@pub.sioc.ac.cn
Yang
C G
CG
Xiong
W N
WN
Wang
J
J
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity*; D004354:Drug Screening Assays, Antitumor / Q000592:standards; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D011719:Pyrazines / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity*; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity*; D014407:Tumor Cells, Cultured / Q000187:drug effects
C434317:2,4-bis(3'-indolyl)pyrimidine; D000970:Antineoplastic Agents; D007211:Indoles; D011719:Pyrazines; D011743:Pyrimidines