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Synthesis and preliminary biological evaluation of a new pyridocarbazole derivative covalently linked to a thymidine nucleoside as a potential targeted antitumoral agent. I

Saturnino, Carmela and Buonerba, Mariafrancesca and Boatto, Gianpiero and Pascale, Maria and Moltedo, Ornella and De Napoli, Lorenzo and Montesarchio, Daniela and Lancelot, Jean-Charles and De Caprariis, Paolo (2003) Synthesis and preliminary biological evaluation of a new pyridocarbazole derivative covalently linked to a thymidine nucleoside as a potential targeted antitumoral agent. I. Chemical and Pharmaceutical Bulletin, Vol. 51 (8), p. 971-974. eISSN 1347-5223. Article.

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DOI: 10.1248/cpb.51.971

Abstract

The therapy of human cancer is one of the more pursued goals by medicinal chemistry research. Most of the compounds clinically used as a treatment owe their efficacy to their cytotoxic interaction (direct or indirect) with nuclear DNA. This interaction results in the inhibition of DNA synthesis and the degradation of nucleic strands. Ellipticine is a naturally occurring 6H-pyrido[4,3-b]carbazole alkaloid endowed with antitumor activity, and several ellipticine derivatives have been used in clinical trials. We previously reported some 1,4-dimethyl-9H-carbazole derivatives structurally related to ellipticine. The purpose of our research was to transform the pyridocarbazole in a prodrug so that it would have more penetration in the tumor cells and block their replication. Our prodrug is slowly hydrolyzed in human plasma in the corresponding acid. From these preliminary results, we deduce that our compound can block cellular replication. Our hypothesis is that the antitumoral activity is probably related to the induction of damage to DNA, without cellular lysis in the short term.

Item Type:Article
ID Code:5168
Status:Published
Refereed:Yes
Uncontrolled Keywords:Ellipticine, anticancer, cytotoxicity
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Scienze biomediche
001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:The Pharmaceutical Society of Japan
eISSN:1347-5223
Deposited On:03 Dec 2010 09:02

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