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Quinoxaline chemistry: Part 16: 4-Substituted anilino and 4-substituted phenoxymethyl pyrrolo[1,2-a]quinoxalines and N-[4-(pyrrolo[1,2-a]quinoxalin-4-yl)amino and hydroxymethyl]benzoyl glutamates: synthesis and evaluation of in vitro biological activity

Alleca, Sergio and Corona, Paola and Loriga, Mario and Paglietti, Giuseppe and Loddo, Roberta and Mascia, Valeria and Busonera, Bernardetta and La Colla, Paolo (2003) Quinoxaline chemistry: Part 16: 4-Substituted anilino and 4-substituted phenoxymethyl pyrrolo[1,2-a]quinoxalines and N-[4-(pyrrolo[1,2-a]quinoxalin-4-yl)amino and hydroxymethyl]benzoyl glutamates: synthesis and evaluation of in vitro biological activity. Il Farmaco, Vol. 58 (9), p. 639-650. ISSN 0014-827X. Article.

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DOI: 10.1016/S0014-827X(03)00101-0

Abstract

Twenty eight pyrrolo[1,2-a]quinoxalines bearing at position 4 various substituents related to the moieties present in classical and non classical antifolic agents were prepared and evaluated in vitro for antiproliferative activity. In an in vitro screening performed at NCI, several compounds emerged as potent antiproliferative agents at concentrations ranging between 10 and 100 μM. Interestingly, some of these compounds proved active also against bovine and murine DHFR (Farmaco 53 (1998) 480). More recently, a compound of classical antifolate type has been reported to be a potent inhibitor of hDHFR in vitro (Farmaco 58 (2003) 51). We then synthesized new derivatives that, in our hands, were endowed with in vitro antiproliferative activities as low as 3.4 μM against a panel of cell lines derived from hematological and solid tumours. In addition, a complete screening of cytotoxicity, antiretroviral HIV-1 and antimicrobial activity has been carried out.

Item Type:Article
ID Code:1395
Status:Published
Refereed:Yes
Uncontrolled Keywords:Potential antifolate agents, antiproliferative agents, pyrrolo[1,2-a]quinoxalines
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:© 2003 Éditions scientifiques et médicales Elsevier
Deposited On:18 Aug 2009 10:05

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