Kuo, Gee-Hong published the artcileSynthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors, Computed Properties of 41668-13-7, the main research area is pyridinyltin dichloropyrazine Stille coupling; chloropyrazine pyridine preparation; pyrazine pyridine derivative preparation VEGFR2 ligand; pyridine pyrazine derivative preparation anticancer.
There is much evidence that direct inhibition of the kinase activity of vascular endothelial growth factor receptor-2 (VEGFR-2) will result in the reduction of angiogenesis and the suppression of tumor growth. Palladium-catalyzed C-C bond, C-N bond formation reactions were used to assemble various pyrazine-pyridine biheteroaryls as potent VEGFR-2 inhibitors. Among them, I [R = NH(CH2)4OH, NH(CH2)2NMe2] exhibited the highest kinase selectivity against fibroblast growth factor receptor kinase, platelet-derived growth factor receptor kinase, and glycogen synthase kinase-3. All of these compounds showed good cellular potency to inhibit VEGF-stimulated proliferation of human umbilical vein endothelial cells (HUVEC) but with modest effects on the unstimulated growth of HUVEC. The low inhibition of these compounds to the growth of tumor cell lines, such as HeLa, HCT-116, and A375 further confirms that these VEGFR-2 inhibitors are not cytotoxic agents. The in vivo antitumor activity of I were demonstrated in the A375 human melanoma xenograft nude mice model. Mol. modeling (QSAR anal.) was conducted in an attempt to rationalize the observed structure-activity relationship.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 41668-13-7 belongs to class bromides-buliding-blocks, name is 5-Bromo-6-hydroxynicotinic acid, and the molecular formula is C6H4BrNO3, Computed Properties of 41668-13-7.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary