The author of 《Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors》 were Liu, Ruiqi; Zhang, Zhuqing; Yang, Hong; Zhou, Kaixin; Geng, Meiyu; Zhou, Weicheng; Zhang, Mingming; Huang, Xun; Li, Yingxia. And the article was published in European Journal of Medicinal Chemistry in 2019. HPLC of Formula: 4949-44-4 The author mentioned the following in the article:
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 Ethyl 3-oxopentanoate(cas: 4949-44-4HPLC of Formula: 4949-44-4)
Ethyl 3-oxopentanoate(cas: 4949-44-4) belongs to ketone compounds. They are most widely used as solvents, especially in industries manufacturing explosives, lacquers, paints, and textiles. Ketones are also used in tanning, as preservatives, and in hydraulic fluids.HPLC of Formula: 4949-44-4
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