Hunt, John T.; Mitt, Toomas; Borzilleri, Robert; Gullo-Brown, Johnni; Fargnoli, Joseph; Fink, Brian; Han, Wen-Ching; Mortillo, Steven; Vite, Gregory; Wautlet, Barri; Wong, Tai; Yu, Chiang; Zheng, Xiaoping; Bhide, Rajeev published the article 《Discovery of the Pyrrolo[2,1-f][1,2,4]triazine Nucleus as a New Kinase Inhibitor Template》. Keywords: pyrrolotriazine derivative preparation structure activity VEGF EGFR kinase antitumor.They researched the compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9 ).Reference of 1-Aminopyrrole-2-carboxamide. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:159326-69-9) here.
The pyrrolo[2,1-f][1,2,4]triazine nucleus was identified as a novel kinase inhibitor template which effectively mimics the well-known quinazoline kinase inhibitor scaffold. Attachment of a 4-((3-chloro-4-fluorophenyl)amino) substituent to the template provided potent biochem. inhibitors of the tyrosine kinase activity of EGFR, as well as inhibition of cellular proliferation of the human colon tumor cell line DiFi. Attachment of a 4-((3-hydroxy-4-methylphenyl)amino) substituent provided potent inhibitors of VEGFR-2 which also showed effects on the VEGF-dependent proliferation of human umbilical vein endothelial cells. Biol. activity was maintained with substitution at positions 5 or 6, but not 7, suggesting that the former positions are promising sites for introducing side chains which modulate physicochem. properties. Preliminary inhibition studies with varying ATP concentrations suggest that, like the quinazoline-based kinase inhibitors, the pyrrolotriazine-based inhibitors bind in the ATP pocket.
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Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica