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Optimizing thiadiazole analogues of resveratrol versus three chemopreventive targets.

ABSTRACT: Chemoprevention is an approach to decrease cancer morbidity and mortality through inhibition of carcinogenesis and prevention of disease progression. Although the trans stilbene derivative resveratrol has chemopreventive properties, its action is compromised by weak non-specific effects on many biological targets. Replacement of the stilbene ethylenic bridge of resveratrol with a 1,2,4-thiadiazole heterocycle and modification of the substituents on the two aromatic rings afforded potential chemopreventive agents with enhanced potencies and selectivities when evaluated as inhibitors of aromatase and NF-?B and inducers of quinone reductase 1 (QR1).

SUBMITTER: Mayhoub AS

PROVIDER: S-EPMC3248958 | biostudies-literature | 2012 Jan

REPOSITORIES: biostudies-literature

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Optimizing thiadiazole analogues of resveratrol versus three chemopreventive targets.

Mayhoub Abdelrahman S AS Marler Laura L Kondratyuk Tamara P TP Park Eun-Jung EJ Pezzuto John M JM Cushman Mark M

Bioorganic & medicinal chemistry 20110925 1

Chemoprevention is an approach to decrease cancer morbidity and mortality through inhibition of carcinogenesis and prevention of disease progression. Although the trans stilbene derivative resveratrol has chemopreventive properties, its action is compromised by weak non-specific effects on many biological targets. Replacement of the stilbene ethylenic bridge of resveratrol with a 1,2,4-thiadiazole heterocycle and modification of the substituents on the two aromatic rings afforded potential chemo ...[more]

PMID: 22115839

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