Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors
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https://figshare.com/articles/dataset/Discovery_of_a_Dihydroisoquinolinone_Derivative_NVP_CGM097_A_Highly_Potent_and_Selective_MDM2_Inhibitor_Undergoing_Phase_1_Clinical_Trials_in_p53wt_Tumors/2136934
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资源简介：
As a result of our efforts to discover
novel p53:MDM2 protein–protein
interaction inhibitors useful for treating cancer, the potent and
selective MDM2 inhibitor NVP-CGM097 (1) with an excellent
in vivo profile was selected as a clinical candidate and is currently
in phase 1 clinical development. This article provides an overview
of the discovery of this new clinical p53:MDM2 inhibitor. The following
aspects are addressed: mechanism of action, scientific rationale,
binding mode, medicinal chemistry, pharmacokinetic and pharmacodynamic
properties, and in vivo pharmacology/toxicology in preclinical species.
创建时间：
2016-02-13
