Anaplastic lymphoma kinase (ALK) is a validated therapeutic target for treating echinoderm microtubule-associated protein-like 4 (EML4)-ALK positive non-small cell lung cancer (NSCLC). We synthesized a series of 1,3,5-triazine derivatives and identified ASP3026 (14a) as a potent and selective ALK inhibitor. In mice xenografted with NCI-H2228 cells expressing EML4-ALK, once-daily oral administration of 14a demonstrated dose-dependent antitumor activity. Here, syntheses and structure-activity relationship (SAR) studies of 1,3,5-triazine derivatives are described.
Terpenes Terpenes U 0200 Biological Activities of α-Mangostin Derivatives Against Acidic Sphingomyelinase. -The synthesis and inhibitory activities against sphingomyelinase of deprenyl and benzophenone-type congeners of α-mangostin are presented. -(HAMADA, M.; IIKUBO, K.; ISHIKAWA, Y.; IKEDA, A.; UMEZAWA, K.; NISHIYAMA*, S.; Bioorg. Med.
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