On October 15, 2019, Liu, Ruiqi; Zhang, Zhuqing; Yang, Hong; Zhou, Kaixin; Geng, Meiyu; Zhou, Weicheng; Zhang, Mingming; Huang, Xun; Li, Yingxia published an article.Computed Properties of 517-23-7 The title of the article was Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors. And the article contained the following:
In order to find potent p300 inhibitors with good drug-like properties, C646 was chosen as the lead compound and a series of new p300 inhibitors were designed based on the principle of bioisosterism and reasonable scaffold hopping and the structure-activity relationship was systematically explored. Ten of them were found to show comparable inhibitory activity as C646. The most potent pyrazolylidene compound, e.g., I (IC50 = 0.16 μM), showed better p300 inhibitory activity than C646 with improved drug-like properties. Western blotting experiment confirmed that pyrazolylidene compound, e.g., I could reduce the level of H3K27 acetylation more significantly than C646. Further cellular assay indicated that it could inhibit the proliferation of human breast ductal carcinoma cell T47D and human breast cancer cell MCF7 with the IC50 values of 5.08 μM and 22.54 μM, resp. Docking study of pyrazolylidene compound, e.g., I with p300 protein showed the possible reasons for its higher inhibition activity. Thus, pyrazolylidene compound, e.g., I might be with potential for development as a novel epigenetic agent targeting p300. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Computed Properties of 517-23-7
The Article related to phenylazolylidene phenylheteroarene preparation histone acetyltransferase p300 inhibition sar docking, c646, epigenetics, sensitive tumor cell proliferation, structure-activity relationship, p300 inhibitors and other aspects.Computed Properties of 517-23-7
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