【摘 要】
：
Phosphoinositide 3-kinases(PI3Ks) are lipid kinases which have been found in many cellular processes,including glucose homeostasis,metabolism,survival,proli
【机 构】
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ZJU-ENS Joint laboratory of Medicinal Chemistry
【出 处】
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第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
Phosphoinositide 3-kinases(PI3Ks) are lipid kinases which have been found in many cellular processes,including glucose homeostasis,metabolism,survival,proliferation and differentiation.While amplification or over-expression of PI3Ks commonly occurs in various type of cancers.Among the class Ⅰ PI3Ks,PI3Kαhas been well established as a promising target for cancer therapy due to the prevalent mutation and amplification of PIK3CA,which leads intense effort in recent years to develop PI3Kα inhibitors.A series of novel arylsulfonyl quinoxaline derivatives were synthesized based on the lead compounds XL-765 and XL-147 which are currently in phase Ⅰ/Ⅱ and Ⅱ trials for cancer treatment.
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