158580-95-1Relevant articles and documents
Pyrimidine amine compound, and preparation method and application thereof
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Paragraph 0455-0456; 0457-0458, (2020/07/02)
The invention discloses a polycyclic compound, and a preparation method and an application thereof. The invention provides the polycyclic compound represented by formula I, or a pharmaceutically acceptable salt thereof. The compound has a relatively good inhibition effect on CDK7.
NITROGENATED HETEROCYCLIC COMPOUND AND AGRICULTURAL OR HORTICULTURAL FUNGICIDE
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, (2014/03/25)
An agricultural or horticultural fungicide contains as an active ingredient thereof at least one compound selected from the group consisting of nitrogenated heterocyclic compounds represented by formula (I) (wherein, R represents a group represented by CR
Synthesis and SAR study of novel 3,3-diphenyl-1,3-dihydroindol-2-one derivatives as potent eIF2·GTP·Met-tRNAiMet ternary complex inhibitors
Denoyelle, Séverine,Chen, Ting,Yang, Hongwei,Chen, Limo,Zhang, Yingzhen,Halperin, José A.,Aktas, Bertal H.,Chorev, Michael
, p. 537 - 553 (2013/10/22)
The growing recognition of inhibition of translation initiation as a new and promising paradigm for mechanism-based anti-cancer therapeutics is driving the development of potent, specific, and druggable inhibitors. The 3,3-diaryloxindoles were recently reported as potential inhibitors of the eIF2·GTP·Met-tRNAiMet ternary complex assembly and 3-{5-tert-butyl-2-hydroxyphenyl}-3-phenyl-1,3-dihydro-2H-indol-2- one #1181 was identified as the prototypic agent of this chemotype. Herein, we report our continuous effort to further develop this chemotype by exploring the structural latitude toward different polar and hydrophobic substitutions. Many of the novel compounds are more potent than the parent compound in the dual luciferase ternary complex reporter assay, activate downstream effectors of reduced ternary complex abundance, and inhibit cancer cell proliferation in the low μM range. Moreover, some of these compounds are decorated with substituents that are known to endow favorable physicochemical properties and as such are good candidates for evaluation in animal models of human cancer.