Design and Synthesis of Pironetin Analogue/Colchicine Hybrids and Study of Their Cytotoxic Activity and Mechanisms of Interaction with Tubulin
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Títol
Design and Synthesis of Pironetin Analogue/Colchicine Hybrids and Study of Their Cytotoxic Activity and Mechanisms of Interaction with TubulinAutoria
Data de publicació
2014-11Editor
American Chemical SocietyCita bibliogràfica
VILANOVA, Concepción, et al. Design and Synthesis of Pironetin Analogue/Colchicine Hybrids and Study of Their Cytotoxic Activity and Mechanisms of Interaction with Tubulin. Journal of medicinal chemistry, 2014, 57.24: 10391-10403.Tipus de document
info:eu-repo/semantics/articleVersió de l'editorial
http://pubs.acs.org/doi/abs/10.1021/jm501112qParaules clau / Matèries
Resum
We here report the synthesis of a series of 12 hybrid molecules composed of a colchicine moiety and a pironetin analogue fragment. The two fragments are connected through an ester–amide spacer of variable length. The ... [+]
We here report the synthesis of a series of 12 hybrid molecules composed of a colchicine moiety and a pironetin analogue fragment. The two fragments are connected through an ester–amide spacer of variable length. The cytotoxic activities of these compounds and their interactions with tubulin have been investigated. Relations between the structure and activity are discussed. Since the spacer is not long enough to permit a simultaneous binding of the hybrid molecules to the colchicine and pironetin sites on tubulin, a further feature investigated was whether these molecules would interact with the latter through the pironetin end (irreversible covalent binding) or through the colchicine end (reversible noncovalent binding). It has been found that binding to tubulin may take place preferentially at either of these ends depending on the length of the connecting spacer. [-]
Publicat a
J. Med. Chem., 2014, 57 (24)Drets d'accés
Copyright © 2014 American Chemical Society
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