931111-57-8Relevant academic research and scientific papers
Structure-based design and synthesis of 2,4-diaminopyrimidines as EGFR L858R/T790M selective inhibitors for NSCLC
Chen, Lingfeng,Fu, Weitao,Feng, Chen,Qu, Rong,Tong, Linjiang,Zheng, Lulu,Fang, Bo,Qiu, Yinda,Hu, Jie,Cai, Yuepiao,Feng, Jianpeng,Xie, Hua,Ding, Jian,Liu, Zhiguo,Liang, Guang
supporting information, p. 510 - 527 (2017/10/10)
Mutated epidermal growth factor receptor (EGFR) is a major driver of non-small cell lung cancer (NSCLC). The EGFRT790M secondary mutation has become a leading cause of clinically-acquired resistance to gefitinib and erlotinib. Herein, we present a structure-based design approach to increase the potency and selectivity of the previously reported reversible EGFR inhibitor 7, at the kinase and cellular levels. Three-step structure-activity relationship exploration led to promising compounds 19e and 19h with unique chemical structure and binding mode from the other third-generation tyrosine kinase inhibitors. In a human NSCLC xenograft model, 19e and 19h exhibited dose-dependent tumor growth suppression without toxicity. These selective inhibitors are promising drug candidates for EGFRT790M-driven NSCLC.
NOVEL AMINE DERIVATIVE OR SALT THEREOF
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Paragraph 0835-0836, (2015/11/11)
A novel amine derivative expressed by general formula (1) (in the formula: G1, G2, and G3 are the same or different and represent CH or a nitrogen atom; R1 represents a chlorine atom, an optionally-substituted C3-8 cycloalkyl group, or the like; R2 represents -COOR5 (in the formula, R5 represents a hydrogen atom or a carboxyl protective group), or the like; R3 represents a hydrogen atom, or the like; and R4 represents an optionally-substituted condensed bicyclic hydrocarbon group, an optionally-substituted bicyclic heterocyclic group, or the like), or a salt thereof is useful in procedures such as the treatment or prevention of conditions related to excessive keratinocyte proliferation.
QUINAZOLINE DERIVATIVES AS ANTICANCER AGENTS
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Page/Page column 76, (2008/06/13)
A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blood
THIA-TETRAAZAACENAPHTHYLENE KINASE INHIBITORS
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Page/Page column 99-100, (2008/06/13)
The present invention is directed to novel thia-tetraazaacenaphthylene compounds of Formula (I): and pharmaceutically acceptable forms thereof and their synthesis and use as inhibitors of ATP-protein kinase interactions.
