958253-44-6Relevant articles and documents
SUBSTITUTED PYRIDINONE-CONTAINING TRICYCLIC COMPOUNDS, AND METHODS USING SAME
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, (2018/05/24)
The present invention includes substituted pyridinone-containing tricyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infection in a patient. In certain embodiments, the compounds and compositions of the invention inhibit and/or reduce HBsAg secretion.
Identification of a new series of potent diphenol HSP90 inhibitors by fragment merging and structure-based optimization
Ren, Jing,Li, Jian,Wang, Yueqin,Chen, Wuyan,Shen, Aijun,Liu, Hongchun,Chen, Danqi,Cao, Danyan,Li, Yanlian,Zhang, Naixia,Xu, Yechun,Geng, Meiyu,He, Jianhua,Xiong, Bing,Shen, Jingkang
, p. 2525 - 2529 (2014/05/20)
Heat shock protein 90 (HSP90) is a molecular chaperone to fold and maintain the proper conformation of many signaling proteins, especially some oncogenic proteins and mutated unstable proteins. Inhibition of HSP90 was recognized as an effective approach to simultaneously suppress several aberrant signaling pathways, and therefore it was considered as a novel target for cancer therapy. Here, by integrating several techniques including the fragment-based drug discovery method, fragment merging, computer aided inhibitor optimization, and structure-based drug design, we were able to identify a series of HSP90 inhibitors. Among them, inhibitors 13, 32, 36 and 40 can inhibit HSP90 with IC50 about 20-40 nM, which is at least 200-fold more potent than initial fragments in the protein binding assay. These new HSP90 inhibitors not only explore interactions with an under-studied subpocket, also offer new chemotypes for the development of novel HSP90 inhibitors as anticancer drugs.
1,3-DIHYDROISOINDOLE DERIVATIVES
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Page/Page column 18, (2010/12/29)
Novel 1,3-dihydroisoindole derivatives of the formula (I), in which R1-R3 have the meanings indicated in claim 1, areHSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.