Potent N-(1,3-Thiazol-2-yl)pyridin-2-amine Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitors with Excellent Pharmacokinetics and Low Affinity for the hERG Ion Channel was written by Bilodeau, Mark T.;Balitza, Adrienne E.;Koester, Timothy J.;Manley, Peter J.;Rodman, Leonard D.;Buser-Doepner, Carolyn;Coll, Kathleen E.;Fernandes, Christine;Gibbs, Jackson B.;Heimbrook, David C.;Huckle, William R.;Kohl, Nancy;Lynch, Joseph J.;Mao, Xianzhi;McFall, Rosemary C.;McLoughlin, Debra;Miller-Stein, Cynthia M.;Rickert, Keith W.;Sepp-Lorenzino, Laura;Shipman, Jennifer M.;Subramanian, Raju;Thomas, Kenneth A.;Wong, Bradley K.;Yu, Sean;Hartman, George D.. And the article was included in Journal of Medicinal Chemistry in 2004.Formula: C9H6ClNS This article mentions the following:
A series of N-(1,3-thiazol-2-yl)pyridin-2-amine KDR kinase inhibitors have been developed that possess optimal properties. Compounds have been discovered that exhibit excellent in vivo potency. The particular challenges of overcoming hERG binding activity and QTc increases in vivo in addition to achieving good pharmacokinetics have been accomplished by discovering a unique class of amine substituents. These compounds have a favorable kinase selectivity profile that can be accentuated with appropriate substitution. In the experiment, the researchers used many compounds, for example, 2-Chloro-5-phenylthiazole (cas: 329794-40-3Formula: C9H6ClNS).
2-Chloro-5-phenylthiazole (cas: 329794-40-3) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Formula: C9H6ClNS
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica