T790米
心脏毒性
奥西默替尼
化学
药理学
赫尔格
组合化学
体外
IC50型
立体化学
医学
表皮生长因子受体
生物化学
毒性
受体
内科学
埃罗替尼
有机化学
钾通道
吉非替尼
作者
Harun Patel,M. Azim Ansari,Rahul Pawara,Iqrar Ansari,Harsha Jadhav,Sanjay J. Surana
标识
DOI:10.1080/10799893.2018.1557207
摘要
Cardiotoxicity is one amongst the adverse effect of Osimertinib delineate in clinical trials and related to escalating doses. To triumph over the drawbacks of Osimertinib, in this study, we tend to delineate the design, synthesis, in vitro biological analysis of a series of novel reversible selective T790M inhibitors with minimal cardiotoxicity. Amongst the virtually sorted compounds; compound 18 and 74 have been located to be the foremost active compounds of the series with IC50 value of 0.88, 0.92 μM in cellular assay and 0.56, 0.62 μM in enzymatic assay, against double mutant L858R/T790M EGFR. Additionally, they showed much less affinity toward wild-type (WT)-EGFR with minimal cardiotoxicity.
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