[EN] INHIBITORS OF MYC AND USES THEREOF [FR] INHIBITEURS DE MYC ET LEURS UTILISATIONS
摘要:
Disclosed are substituted heterocyclic compounds and proteolysis-targeting chimeric molecules (PROTACs). The substituted heterocycles disclosed herein are shown to be useful in inhibiting c-MYC. The disclosed PROTACs are shown to induce degradation of c-MYC protein. The substituted heterocyclic compounds and proteolysis-targeting chimeric molecules (PROTACs) disclosed, herein may be utilized as therapeutics for treating cancer and cell proliferative disorders.
[EN] BENZOTHIOPHENE DERIVATIVES AS ESTROGEN RECEPTOR INHIBITORS<br/>[FR] DÉRIVÉS BENZOTHIOPHÈNE COMME INHIBITEURS DU RÉCEPTEUR DES ŒSTROGÈNES
申请人:GLAXOSMITHKLINE IP DEV LTD
公开号:WO2015000867A1
公开(公告)日:2015-01-08
A compound of formula (I), or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
Radiolabeled pyridinyl analogues of dibenzylideneacetone as β-amyloid imaging probes
作者:Xiaomei Cui、Xiaoyang Zhang、Cheng Peng、Jiapei Dai、Boli Liu、Mengchao Cui
DOI:10.1039/c6ra05168e
日期:——
In continuation of our investigation of the dibenzylideneacetone scaffold as Aβ imaging probes, a series of derivatives containing pyridine rings with lower lipophilicity was synthesized and evaluated.
在我们对二苯基丙酮骨架作为Aβ成像探针的研究中,合成并评估了一系列含有吡啶环且疏水性较低的衍生物。
Synthesis and Conformational Analysis of Macrocyclic Dihydroxystilbenes Linked between thepara–para Positions
3-oxapentamethylene or hexamethylene chain. The key macrocyclization step was achieved in moderate yields by using an intramolecular McMurry pinacolcoupling of linked aromatic dialdehydes, except for the nitro-substituted compounds. The relative stereochemistry of the isomeric pinacols was determined by a combination of spectroscopic, chemical derivatization, and molecular-modeling approaches. The NMR
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents
作者:Nishad Thamban Chandrika、Sanjib K. Shrestha、Huy X. Ngo、Sylvie Garneau-Tsodikova
DOI:10.1016/j.bmc.2016.06.010
日期:2016.8
pathogenic fungal strains have resulted in an increase in demand for new antifungal agents. Various heterocyclic scaffolds with different mechanisms of action against fungi have been investigated in the past. Herein, we report the synthesis and antifungal activities of 18 alkylated mono-, bis-, and trisbenzimidazole derivatives, their toxicities against mammalian cells, as well as their ability to induce