Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity.
Bioorganic & Medicinal Chemistry Letters（2006）
摘要
A series of 27 isoquinoline–pyridine-based derivatives were synthesized and evaluated as protein kinase B/Akt antagonists. An amino analog (R5=NH2) demonstrated good efficacy in a mouse MiaPaCa-2 xenograft model, but with accompanying toxicity.
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关键词
Akt inhibitor,Protein kinase B,PKB,GSK3,FL5.12-Akt,Anticancer
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