Discovery of a Potent and Selective PI3Kδ Inhibitor (<i>S</i>)-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4<i>H</i>-quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models.
作者:
主题词
动物(Animals);抗肿瘤药(Antineoplastic Agents);细胞系, 肿瘤(Cell Line, Tumor);I类磷脂酰肌醇3-激酶类(Class I Phosphatidylinositol 3-Kinases);狗(Dogs);药物发现(Drug Discovery);女(雌)性(Female);血液肿瘤(Hematologic Neoplasms);人类(Humans);男(雄)性(Male);小鼠(Mice);小鼠, 近交BALB C(Mice, Inbred BALB C);小鼠, 近交NOD(Mice, Inbred NOD);小鼠, SCID(Mice, SCID);分子结构(Molecular Structure);喹嗪类(Quinolizines);大鼠, Sprague-Dawley(Rats, Sprague-Dawley);构效关系(Structure-Activity Relationship);异种移植模型抗肿瘤试验(Xenograft Model Antitumor Assays)
DOI
10.1021/acs.jmedchem.0c01264
PMID
33297683
发布时间
2021-02-03
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Journal of medicinal chemistry
14700-14723页
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