309732-78-3Relevant academic research and scientific papers
Synthesis and Biological Evaluation of N-aryl-4-aryl-1,3-Thiazole-2-Amine Derivatives as Direct 5-Lipoxygenase Inhibitors
Suh, Jeehee,Yum, Eul Kgun,Cheon, Hyae Gyeong,Cho, Young Sik
experimental part, p. 89 - 98 (2012/08/29)
Biological evaluation of N-aryl-4-aryl-1,3-thiazole-2-amine derivatives was examined for anti-inflammatory activity in in vitro and in vivo assays. The thiazole compounds showed direct inhibition of 5-lipoxygenase (LOX) that is a key enzyme of leukotrienes synthesis and involved in the inflammation-related diseases, including asthma and rheumatoid arthritis. To optimize biological activity, we synthesized 1,3-thiazole-2-amine derivatives and investigated for structure and activity relationship. Especially, N-(3,5-dimethylphenyl)-4-(4-chlorophenyl)-1,3-thiazole-2-amine was shown to have a potent anti-inflammatory activity as a 5-LOX inhibitor.
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
scheme or table, p. 1677 - 1679 (2010/07/03)
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.
