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Synthesis and antiproliferative activity of 3-aryl-2-[1H(2H)-benzotriazol-1(2)-yl]acrylonitriles variously substituted: Part 4

Carta, Antonio and Palomba, Michele Francesco Luigi and Boatto, Gianpiero and Busonera, Bernardetta and Murreddu, Marta and Loddo, Roberta (2004) Synthesis and antiproliferative activity of 3-aryl-2-[1H(2H)-benzotriazol-1(2)-yl]acrylonitriles variously substituted: Part 4. Il Farmaco, Vol. 59 (8), p. 637-644. ISSN 0014-827X. Article.

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DOI: 10.1016/j.farmac.2004.03.004

Abstract

A new series of variously substituted 3-aryl-2-[1H(2H)-benzotriazol-1(2)-yl]acrylonitriles was synthesized and tested for antiproliferative and antitubercular activity as part of our continuing research program in the antimicrobial and antitumor fields. The most cytotoxic derivatives (5a,g,i,j,l and 7b) (CC50 < 3.0 μM against MT-4 cells) were evaluated against a panel of human cell lines derived from hematological and solid tumors, using 6-mercaptopurine (6-MP) and etoposide as reference drugs. In particular, E-2-(5,6-dimethyl-1H-benzotriazol-1-yl)-3-(3-nitrophenyl)acrylonitrile (5g) resulted more potent than 6-MP on all cell lines, even if 2–14-fold less potent than etoposide. In the antitubercular screening, the derivatives 5i,j and 7e showed moderate activity against some resistant strains of Mycobacterium tested.

Item Type:Article
ID Code:4433
Status:Published
Refereed:Yes
Uncontrolled Keywords:3-Aryl-2-(1H(2H)-benzotriazol-1(2)-yl)acrylonitriles, antiproliferative activity, antitubercular screening, SAR
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Elsevier
ISSN:0014-827X
Copyright Holders:© 2004 Elsevier SAS
Deposited On:31 Aug 2010 18:42

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