Isoindolo[2,1-c]benzo[1,2,4]triazines:: A new ring system with antiproliferative activity

被引：45

作者：

Diana, Patrizia ^{[1
]}

Martorana, Annamaria ^{[1
]}

Barraja, Paola ^{[1
]}

Lauria, Antonino ^{[1
]}

Montalbano, Alessandra ^{[1
]}

Almerico, Anna Maria ^{[1
]}

Dattolo, Gaetano ^{[1
]}

Cirrincione, Girolamo ^{[1
]}

机构：

[1] Univ Palermo, Dipartimento Farmacochim Tossicol & Biol, I-90123 Palermo, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 01期

关键词：

isoindolo-benzotriazine; antiproliferative activity; 3D-mind;

D O I：

10.1016/j.bmc.2006.09.054

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：

A series of isoindolo-benzo-triazines of type 4 was obtained by diazotization of 2-(2-aminoaryl)-1-cyanoisoindoles 3a-j All the synthesized derivatives were screened by the National Cancer Institute (NCI, Bethesda, USA), for in vitro antitumor activity against a 3-human cancer cell line panel consisting of MCF7 (breast), NCI-H460 (lung), and SF-268 (CNS). Derivatives 4a, f, i, j were selected to be evaluated in the full panel of about 50 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity generally in the micromolar range. The most sensitive cell lines were: MOLT-4 and SR of the leukemia subpanel, A549/ATCC and EKVX of the nonsmall cell lung subpanel, COLO-205 of the colon cancer subpanel, LOX IMVI of the Melanoma subpanel, OVCAR-8 of the ovarian cancer subpanel, and MCF7, BT-549 of the breast cancer subpanel. (c) 2006 Elsevier Ltd. All rights reserved.

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页码：343 / 349

页数：7

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