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Synthesis and cytotoxic activities of pyrrole[2,3-d]pyridazin-4-one derivatives

Murineddu, Gabriele and Cignarella, Giorgio and Chelucci, Giorgio Adolfo and Loriga, Giovanni and Pinna, Gérard Aimé (2002) Synthesis and cytotoxic activities of pyrrole[2,3-d]pyridazin-4-one derivatives. Chemical and Pharmaceutical Bulletin, Vol. 50 (6), p. 754-759. eISSN 1347-5223. Article.

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1-Methyl-2-phenyl (1) and 1,3-dimethyl-2-phenyl (2) -substituted pyrrole[2,3-d]pyridazinones, as well as their tetracyclic analogues 3—6, were synthesized and evaluated in vitro by the National Cancer Institute against 60 human tumor cell lines derived from nine cancer cell types. Biological results showed that the antitumor activities of these compounds were related to the planarity of their ring systems with potency increasing in the order 2<4 5<6<3. Among them, the most potent compound 3 showed significant cell line cytotoxicity, particularly against the renal cancer subpanel [GI50 (µM) 5.07] and displayed significant potency [GI50 (µM) 3.04—4.32] against MOLT-4, SR (leukemia), NCI-H460 (non-small cell lung), HCT-116 (colon), and SF-295 (CNS) cancer cells, respectively.

Item Type:Article
ID Code:379
Uncontrolled Keywords:Pyrrole[2,3-d]pyridazin-4-one derivative, cytotoxic activity, structure–activity relationship
Subjects:Area 03 - Scienze chimiche > CHIM/06 Chimica organica
Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Chimica
001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:The Pharmaceutical Society of Japan
Deposited On:18 Aug 2009 10:02

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