Ding, Hong; Pei, Yuan; Li, Yuanqing; Xu, Wen; Mei, Lianghe; Hou, Zeng; Guang, Yiman; Cao, Liyuan; Li, Peizhuo; Cao, Haijing; Bian, Jinlei; Chen, Kaixian; Luo, Cheng; Zhou, Bing; Zhang, Ting; Li, Zhiyu; Yang, Yaxi published an article in 2021. The article was titled 《Design, synthesis and biological evaluation of a novel spiro oxazolidinedione as potent p300/CBP HAT inhibitor for the treatment of ovarian cancer》, and you may find the article in Bioorganic & Medicinal Chemistry.HPLC of Formula: 128071-75-0 The information in the text is summarized as follows:
Histone acetylation is one of the most essential parts of epigenetic modification, mediating a variety of complex biol. functions. In these procedure, p300/CBP could catalyze the acetylation of lysine 27 on histone 3 (H3K27ac), and had been reported to mediate tumorigenesis and development in a variety of tumors by enhancing chromatin transcription activity. Ovarian cancer, as an extremely malignant tumor, has also been observed to undergo abnormal acetylation of histones. However, whether the treatment of ovarian cancer could be achieved by inhibiting the acetylation activity of p300/CBP on H3K27 has not been well investigated. In this article, we modified the structure of p300/CBP HAT domain inhibitor A-485 and obtained a highly active small mol. known as 13f, which has an IC50 value of 0.49 nM for inhibiting the in vitro enzyme activity of p300, as well as the anti-proliferation IC50 value on ovarian cancer cell line OVCAR-3 was 153 nM. In addition, 13f had strong acetylase family selectivity, good metabolic stability and promising in vivo anti-tumor activity in OVCAR-3 xenograft model. The discovery of 13f revealed a more active chem. entity of the HATs domain of p300/CBP and provided a novel idea for the application of epigenetic inhibitors in the treatment of ovarian cancer. The results came from multiple reactions, including the reaction of 2-Bromonicotinaldehyde(cas: 128071-75-0HPLC of Formula: 128071-75-0)
2-Bromonicotinaldehyde(cas: 128071-75-0) belongs to pyridine. When pyridine is adsorbed on oxide surfaces or in porous materials, the following species are commonly observed: (i) pyridine coordinated to Lewis acid sites, (ii) pyridine H-bonded to weakly acidic hydroxyls, and (iii) protonated pyridine. At high coverage, physisorbed pyridine and protonated dimers can also be observed.HPLC of Formula: 128071-75-0