138420-09-4Relevant articles and documents
Optimization of Peptidomimetics as Selective Inhibitors for the β-Catenin/T-Cell Factor Protein-Protein Interaction
Wang, Zhen,Zhang, Min,Wang, Jin,Ji, Haitao
supporting information, p. 3617 - 3635 (2019/03/29)
The β-catenin/T-cell factor (Tcf) protein-protein interaction (PPI) plays a critical role in the β-catenin signaling pathway which is hyperactivated in many cancers and fibroses. Based on compound 1, which was designed to target the Tcf4 G13ANDE17 binding site of β-catenin, extensive structure-activity relationship studies have been conducted. As a result, compounds 53 and 57 were found to disrupt the β-catenin/Tcf PPI with the Ki values of 0.64 and 0.44 μM, respectively, and exhibit good selectivity for β-catenin/Tcf over β-catenin/E-cadherin and β-catenin/adenomatous polyposis coli (APC) PPIs. The 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) cell viability assays revealed that 56, the ethyl ester of 53, was more potent than 53 in inhibiting viability of most of the Wnt/β-catenin hyperactive cancer cells. Further cell-based studies indicated that 56 disrupted the β-catenin/Tcf PPI without affecting the β-catenin/E-cadherin and β-catenin/APC PPIs, suppressed transactivation of Wnt/β-catenin signaling in dose-dependent manners, and inhibited migration and invasiveness of Wnt/β-catenin-dependent cancer cells.
Cs2CO3-promoted defluorination and functionalization of α-CF3 carbonyl compounds in the presence of: N -, O -, and/or S -nucleophiles
Wu, Yue,Zhang, Bingbing,Zheng, Yinying,Wang, Yuheng,Lei, Xinsheng
, p. 16019 - 16023 (2018/05/22)
A simple, efficient, and mild method for defluorination and functionalization of 3,3,3-trifluoro carbonyl compounds has been developed. In the present method, Cs2CO3 can easily convert α-trifluoromethyl esters, amides, and ketones in
Monoazo or disazo pigments based on (benoxazol-2-yl)- or (benzimidazol-2-yl)-arylacetamides
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, (2008/06/13)
Water-insoluble azo colorants, their preparation and use The invention relates to monoazo and disazo compounds of the formula (I) STR1 in which D is the radical of a carbocyclic or heterocyclic diazo or bisdiazo component, R1 and R2, independently of one another, are each a substituted or unsubstituted aryl or heteroaryl radical, X1 and X2, independently of one another, are each ring-forming ether oxygen or a substituted or unsubstituted imide grouping and n has the value 0 or 1, in which rings A and B, independently of one another, can each be additionally substituted and/or carry substituted or unsubstituted fused rings. These new compounds of the formula (I) are obtained by coupling diazotized amines or diamines of the type D--NH2 or H2 N--D--NH2 with (benzoxazol-2-yl)- or (benzimidazol-2-yl)-arylacetamides. Depending on the presence and length of alkyl chains, the compounds of the formula (I) are suitable for use as pigments, disperse dyes or oil-soluble dyes.