1334212-41-7Relevant academic research and scientific papers
Optimizing thiadiazole analogues of resveratrol versus three chemopreventive targets
Mayhoub, Abdelrahman S.,Marler, Laura,Kondratyuk, Tamara P.,Park, Eun-Jung,Pezzuto, John M.,Cushman, Mark
experimental part, p. 510 - 520 (2012/03/10)
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).
An unexpected synthesis of 3,5-diaryl-1,2,4-thiadiazoles from thiobenzamides and methyl bromocyanoacetate
Mayhoub, Abdelrahman S.,Kiselev, Evgeny,Cushman, Mark
supporting information; experimental part, p. 4941 - 4943 (2011/10/07)
Aryl thioamides undergo very rapid condensation in the presence of methyl bromocyanoacetate to provide quantitative yields of 3,5-diaryl-1,2,4- thiadiazoles with an easy work-up and a high degree of product purity. The method can be scaled up with no loss in efficiency.
