Antitumor agents .174. 2',3',4',5,6,7-substituted 2-phenyl-1,8-naphthyridin-4-ones: Their synthesis, cytotoxicity, and inhibition of tubulin polymerization

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Title:	Antitumor agents .174. 2',3',4',5,6,7-substituted 2-phenyl-1,8-naphthyridin-4-ones: Their synthesis, cytotoxicity, and inhibition of tubulin polymerization
Authors:	Chen, K;Kuo, SC;Hsieh, MC;Mauger, A;Lin, CM;Hamel, E;Lee, KH
Contributors:	藥學院藥化所;UNIV N CAROLINA,SCH PHARM,DIV MED CHEM & NAT PROD,NAT PROD LAB,CHAPEL HILL,NC 27599;CHINA MED COLL,GRAD INST PHARMACEUT CHEM,TAICHUNG 400,TAIWAN;NCI,DRUG SYNTH & CHEM BRANCH,DEV THERAPEUT PROGRAM,DIV CANC TREATMENT DIAG & CTR,NIH,BETHESDA,MD 20892;NCI,MOL PHARMACOL LAB,DIV BASIC SCI,NIH,BETHESDA,MD 20892
Date:	1997
Issue Date:	2010-09-24 15:06:37 (UTC+8)
Publisher:	AMER CHEMICAL SOC
Abstract:	Norcantharidin[3], the demethylated product of cantharidin[1] has been used for the treatment of hepatoma, carcinomas of esophagus and gastric cardia, leukopenia and hepatitis. Since the enzyme xanthine oxidase is involved in the diseases mentioned above, and the reactive oxygen species produced by the enzyme induces DNA damage and oxidative damage of tissues, fourteen cantharidin analogues and cantharidimide derivatives were tested for their effects on xanthine oxidase. The results showed that these compounds, listed in Figure 1, displayed very weak inhibitory effects on xanthine oxidase. Contrary to expectation, disodium cantharidate [2], Norcantharidin [3], dehydronorcantharidin [4], disodium dehydronorcantharidate [5], N-(2-pyridyl) cantharidimide [12], N-(3pyridyl) cantharidimide [13] and N-(4-pyridyl) cantharidimide [14] showed a slight stimulating effect on xanthine oxidase at several concentrations.
Relation:	JOURNAL OF MEDICINAL CHEMISTRY 40(14):2266-2275
Appears in Collections:	[Graduate Institute of Pharmaceutical Chemistry] Journal articles

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