315706-17-3Relevant academic research and scientific papers
2-Anilino-4-aryl-1,3-thiazole inhibitors of valosin-containing protein (VCP or p97)
Bursavich, Matthew G.,Parker, Daniel P.,Willardsen, J. Adam,Gao, Zhong-Hua,Davis, Thaylon,Ostanin, Kirill,Robinson, Rosann,Peterson, Ashley,Cimbora, Daniel M.,Zhu, Ju-Fen,Richards, Burt
, p. 1677 - 1679 (2010)
Valosin-containing protein (VCP; also known as p97) is a member of the AAA ATPase family with a central role in the ubiquitin-degradation of misfolded proteins. VCP also exhibits antiapoptotic function and metastasis via activation of nuclear factor kappa-B signaling pathway. We have discovered that 2-anilino-4-aryl-1,3-thiazoles are potent drug-like inhibitors of this enzyme. The identified compounds show low nanomolar VCP potency, demonstrate SAR trends, and show activity in a mechanism based cellular assay. This series of compounds represents the first steps towards a novel, small molecule VCP inhibitor as a cancer therapeutic.
