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Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation

A series of structurally novel quinazolone-based PI3Kδ-selective inhibitors were designed and synthesized via the approach of conformational restriction. The majority of them exhibited two-digit to single-digit nanomolar IC(50) values against PI3Kδ, along with low micromolar to submicromolar GI(50)...

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Publicado en:Medchemcomm
Autores principales: Ma, Xiaodong, Fang, Fang, Tao, Qiangqiang, Shen, Li, Zhong, Guochen, Qiao, Tao, Lv, Xiaoqing, Li, Jiaming
Formato: Artigo
Lenguaje:Inglês
Publicado: Royal Society of Chemistry 2019
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Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC6431952/
https://ncbi.nlm.nih.gov/pubmed/30996859
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/c8md00556g
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