Ishikawa, Tomoyasu published the artcileDesign and Synthesis of Novel Human Epidermal Growth Factor Receptor 2 (HER2)/Epidermal Growth Factor Receptor (EGFR) Dual Inhibitors Bearing a Pyrrolo[3,2-d]pyrimidine Scaffold, Recommanded Product: 3-Chloro-4-fluoronitrobenzene, the publication is Journal of Medicinal Chemistry (2011), 54(23), 8030-8050, database is CAplus and MEDLINE.
Dual inhibitors of human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives, e.g. I, capable of fitting into the receptors’ ATP binding site. Among the prepared compounds, I showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor growth inhibitory activity. The X-ray cocrystal structures of I with both HER2 and EGFR demonstrated that I interacts with the expected residues in their resp. ATP pockets. Furthermore, reflecting its good oral bioavailability, I exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report I (TAK-285) as a promising candidate for clin. development as a novel HER2/EGFR dual kinase inhibitor.
Journal of Medicinal Chemistry published new progress about 350-30-1. 350-30-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Nitro Compound,Benzene, name is 3-Chloro-4-fluoronitrobenzene, and the molecular formula is C6H3ClFNO2, Recommanded Product: 3-Chloro-4-fluoronitrobenzene.
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