Optimizing thiadiazole analogues of resveratrol versus three chemopreventive targets.

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Mayhoub AS, Marler L, Kondratyuk TP, Park EJ, Pezzuto JM, Cushman M

Optimizing thiadiazole analogues of resveratrol versus three chemopreventive targets.

Bioorg Med Chem. 2012 Jan 1;20(1):510-20. doi: 10.1016/j.bmc.2011.09.031. Epub 2011 Sep 25.

PubMed ID

22115839 [ View in PubMed

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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-kappaB and inducers of quinone reductase 1 (QR1).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Naringenin	Cytochrome P450 19A1	IC 50 (nM)	230	N/A	N/A	Details