2-Phenylthiazole-5-carboxylic Acid Derivative

Nanomolar TRBP inhibition

An orally bioavailable small molecule with sorafenib-comparable efficacy and lower toxicity, blocking the TRBP-Dicer interaction to suppress oncogenic miR-21.

Shi, Hailong · Yu, Jialing · Li, Lingyu · Runze, Li · Peng, Ting · Cheng, Yao · Wang, Tao · Yang, Linhan · Zhao, Wu · Zhang, Guolin · Wang, Fei · Lu, Xiaoxia

Journal of Medicinal Chemistry 2024

Specifications

EC
{'zh': '0.66', 'en': '0.66'} nM
KD
{'zh': '4.78', 'en': '4.78'} nM
IC
{'zh': '2.34', 'en': '2.34'} μM
口服生物利用度
{'zh': '53.9', 'en': ''} %