Phenylthio-derivatives of α-methylene-γ-lactones as pro-drugs of cytotoxic agents

…, P Barbetti, G Grandolini, I Chiappini, V Ambrogi…

文献索引：Fardella, Giuseppe; Barbetti, Paolo; Grandolini, Giuliano; Chiappini, Ione; Ambrogi, Valeria; Scarcia, Vito; Furlani Candiani, Ariella European Journal of Medicinal Chemistry, 1999 , vol. 34, # 6 p. 515 - 523

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被引用次数: 19

摘要

A series of substituted phenylthio-derivatives of grosheimin (1), a natural cytotoxic guaianolide, were investigated with the aim of providing insight into their mechanism of action as cytotoxic agents against KB cell lines. Hydrolysis data, kinetics, in the presence and in the absence of H2O2, and the valuation of lipophilicity were correlated with cytotoxicity values and with Hammett-σ-values of substituents (R) at the thiophenol ring. ...