Safety of 1-Aminopyrrole-2-carboxamide. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 1-Aminopyrrole-2-carboxamide, is researched, Molecular C5H7N3O, CAS is 159326-69-9, about Discovery of the Pyrrolo[2,1-f][1,2,4]triazine Nucleus as a New Kinase Inhibitor Template. Author is 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.
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