Synthesis and biological activity of mustard derivatives of combretastatins

Beatrice Coggiola, Francesca Pagliai, Gianna Allegrone, Armando A. Genazzani, Gian Cesare Tron

Risultato della ricerca: Contributo su rivistaArticolo in rivistapeer review

Abstract

A series of chimeric compounds bearing the combretastatin and the nitrogen mustard cores were synthesized. All the compounds were cytotoxic and inhibited tubulin polymerization. When combretastatin was joined to chlorambucil via an ester linkage, the resultant compound proved to be significantly more potent than the two compounds put together. When combretastatin was joined to nitrogen mustard via an ether linkage or when a true hybrid was synthesized, loss of potency was observed. Nonetheless, these latter compounds appeared to be more efficacious and surprisingly were able to inhibit tubulin depolymerization at high concentrations.

Lingua originaleInglese
pagine (da-a)3551-3554
Numero di pagine4
RivistaBioorganic and Medicinal Chemistry Letters
Volume15
Numero di pubblicazione15
DOI
Stato di pubblicazionePubblicato - 1 ago 2005

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