水溶性磺酰胺类磷脂酰肌醇 3-激酶抑制剂 ZSTK474 类似物的合成与生物评价。
Synthesis and biological evaluation of solubilized sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.
机构信息
Auckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
Auckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand; Maurice Wilkins Centre for Molecular Biodiscovery, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
出版信息
Bioorg Med Chem. 2019 Apr 15;27(8):1529-1545. doi: 10.1016/j.bmc.2019.02.050. Epub 2019 Feb 25.
Replacing one of the morpholine groups of the phosphatidylinositol 3-kinase (PI3K) inhibitor ZSTK474 with a variety of sulfonamide-linked solubilizing substituents produced a new class of active and potent PI3Kα inhibitors, with several derivatives demonstrating high PI3Kα enzyme potency and good cellular potency in two human derived cell lines. The overall results suggest a preference for linear and somewhat flexible solubilizing functions. From this series, compound 16, also known as SN32976, was selected for advanced preclinical evaluation.
用各种磺酰胺连接的增溶取代基取代磷脂酰肌醇 3-激酶 (PI3K) 抑制剂 ZSTK474 中的一个吗啉基团，产生了一类新的具有活性和强效的 PI3Kα 抑制剂，其中几个衍生物在两种源自人类的细胞系中表现出高的 PI3Kα 酶活性和良好的细胞活性。总体结果表明对线性和稍具柔性的增溶功能具有偏好。从这个系列中，化合物 16，也称为 SN32976，被选为先进的临床前评估。
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