Concise Synthesis and Biological Evaluation of a Phorbazole Analogue-B1 Identifies a Multi-Kinase Inhibitor with Anti-AML Activity.
1/5 보강
Phorbazoles are bioactive marine alkaloids whose development is hampered by limited supply.
APA
Chen X, Zhang L, et al. (2026). Concise Synthesis and Biological Evaluation of a Phorbazole Analogue-B1 Identifies a Multi-Kinase Inhibitor with Anti-AML Activity.. Marine drugs, 24(2). https://doi.org/10.3390/md24020063
MLA
Chen X, et al.. "Concise Synthesis and Biological Evaluation of a Phorbazole Analogue-B1 Identifies a Multi-Kinase Inhibitor with Anti-AML Activity.." Marine drugs, vol. 24, no. 2, 2026.
PMID
41745466 ↗
Abstract 한글 요약
Phorbazoles are bioactive marine alkaloids whose development is hampered by limited supply. We report a concise synthesis of the deschloro-phorbazole core via an optimized iodine-catalyzed oxazole annulation (56% yield). This route enabled efficient access to the scaffold and the preparation of analog . showed nanomolar cytotoxicity (IC = 0.04 µM) against MV4-11 leukemia cells by inducing G0/G1 arrest (via cyclin D1/CDK6 downregulation) and apoptosis. As a multi-kinase inhibitor, also potently inhibited endothelial network formation and migration, demonstrating anti-angiogenic activity. This work provides an efficient synthetic strategy and identifies as a promising dual-function anticancer lead compound.
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