Article
Discovery of Pyrazolo[1,5-a]pyrimidine derivative as a potent and selective PI3Kγ/δ dual inhibitor.
European journal of medicinal chemistry - 15 Nov 2023
Liang Xiaofei, Deng Maoqing, Zou Fengming, Qi Ziping, Wang Chun, Liu Juan, Liu Qingwang, Wang Beilei, Qi Shuang, Ge Juan, Yu Hongwei, Wang Aoli, Liu Qingsong, Liu Jing
Abstract excerpt
Phosphoinositol 3-kinases (PI3Ks) γ and δ are primarily expressed in leukocytes and play crucial roles in regulation of the immune system. Dual inhibition of PI3Kγ/δ has emerged as an effective approach to regulate the tumor microenvironment. Here, we report the exploration of structure-activity relationship optimization which led to the discovery of a potent PI3Kγ/δ dual inhibitor 15u (IHMT-PI3K-455). 15u...
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