Heterocyclic and phenyl double-bond-locked combretastatin analogues possessing potent apoptosis-inducing activity in HL60 and in MDR cell lines

…, R Rondanin, L Piccagli, R Baruchello…

文献索引：Roberti, Marinella; Pizzirani, Daniela; Simoni, Daniele; Rondanin, Riccardo; Baruchello, Riccardo; Bonora, Caterina; Buscemi, Filippo; Grimaudo, Stefania; Tolomeo, Manlio Journal of Medicinal Chemistry, 2003 , vol. 46, # 16 p. 3546 - 3554

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被引用次数: 107

摘要

Two new series of combretastatin (CA-4) analogues have been prepared. The alkenyl motif of CA-4 was replaced either by a five-membered heterocyclic (isoxazoline or isoxazole) or by a six-membered ring (pyridine or benzene). The new compounds have been evaluated for their effects on tubulin assembly and for cytotoxic and apoptotic activities. Five compounds (18b, 20a, 21a, 34b, and 35b) demonstrated an attractive profile of cytotoxicity ...