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

被引：105

作者：

Jiang, B ^{[1
]}

Yang, CG ^{[1
]}

Xiong, WN ^{[1
]}

Wang, J ^{[1
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2001年 / 9卷 / 05期

关键词：

D O I：

10.1016/S0968-0896(00)00337-0

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 muM. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1149 / 1154

页数：6

共 20 条

[1]

ALVAREZ M, 1991, HETEROCYCLES, V32, P1391

[2]

BRACHWITZ VH, 1969, J PRAKT CHEM, V311, P40

[3]

Camerino B., 1960, GAZZ CHIM ITAL, V90, P1807

[4] Indole alkaloids from the tunicate Aplidium meridianum [J].

Franco, LH ;

Joffé, EBD ;

Puricelli, L ;

Tatian, M ;

Seldes, AM ;

Palermo, JA .

JOURNAL OF NATURAL PRODUCTS, 1998, 61 (09) :1130-1132

[5]

GREVER MR, 1992, SEMIN ONCOL, V19, P622

[6] Syntheses and biological activities of bis(3-indolyl)thiazoles, analogues of marine bis(indole)alkaloid nortopsentins [J].

Gu, XH ;

Wan, XZ ;

Jiang, B .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (04) :569-572

[7] Syntheses and cytotoxicity evaluation of bis(indolyl)thiazole, bis(indolyl)pyrazinone and bis(indolyl)pyrazine: Analogues of cytotoxic marine bis(indole) alkaloid [J].

Jiang, B ;

Gu, XH .

BIOORGANIC & MEDICINAL CHEMISTRY, 2000, 8 (02) :363-371

[8] Syntheses of bis(3′-indolyl)-2(1H)-pyrazinones [J].

Jiang, B ;

Gu, XH .

HETEROCYCLES, 2000, 53 (07) :1559-1568

[9] Synthesis of indolylpyrimidines via cross-coupling of indolylboronic acid with chloropyrimidines:: Facile synthesis of meridianin D [J].

Jiang, B ;

Yang, CG .

HETEROCYCLES, 2000, 53 (07) :1489-1498

[10]

Kawasaki I, 1996, CHEM PHARM BULL, V44, P1831

← 1 2 →