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研究人员设计合成STAT3和HDAC双通路抑制剂用于治疗实体肿瘤,PK实验通过BOBSport进行

2023-07-05
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The inhibition of HDACs will lead to compensated activation of a notorious cancer-related drug target, STAT3, in breast cancer through a cascade, which probably limits the anti-proliferation effect of HDAC inhibitors in solid tumors. 

Herein, researchers synthesized a series of potent pterostilbene hydroxamic acid derivatives with dual-target inhibition activity. 

The pharmacokinetic experiment in SD Rats was carried out by Medicilon.

Reference:

Yuhao Ren, et al. Discovery of STAT3 and Histone Deacetylase (HDAC) Dual-Pathway Inhibitors for the Treatment of Solid Cancer. J Med Chem. 2021 Jun 10;64(11):7468-7482. doi: 10.1021/acs.jmedchem.1c00136. 

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