1. Academic Validation
  2. Optimizing thiadiazole analogues of resveratrol versus three chemopreventive targets

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.
Abdelrahman S Mayhoub 1 Laura Marler Tamara P Kondratyuk Eun-Jung Park John M Pezzuto Mark Cushman
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy and the Purdue Center for Cancer Research, Purdue University, West Lafayette, IN 47907, USA.
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-κB and inducers of quinone reductase 1 (QR1).

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