Synthesis of Thicolchicine-Based Conjugates: Investigation towards Bivalent Tubulin/Microtubules Binders
Articolo
Data di Pubblicazione:
2019
Citazione:
Synthesis of Thicolchicine-Based Conjugates: Investigation towards Bivalent Tubulin/Microtubules Binders / E. Bonandi, F. Foschi, C. Marucci, F. Dapiaggi, M. Sironi, S. Pieraccini, M.S. Christodoulou, F. de Asís Balaguer, J.F. Díaz, N. Zidar, D. Passarella. - In: CHEMPLUSCHEM. - ISSN 2192-6506. - 84:1(2019 Jan), pp. 98-102. [10.1002/cplu.201800497]
Abstract:
Four different hybrid compounds have been efficiently synthesized by conjugation of deacetylthiocolchicine with pironetin-inspired derivatives. The modest bioactivity and the apparent absence of interaction with α-tubulin is explained by a posteriori in silico investigation, which suggests a relevant distance between the thiocolchicine binding site and the proper pocket on the α-tubulin. The modest activity on resistant cells suggested that the lipophilic nature of the linker used renders the resulting compounds better substrates for p-Gp efflux pumps. The study better clarifies the design of bivalent compounds that target hetero tubulin/microtubules.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
bivalent binders; microtubules; pironetin; thiocolchicine; tubulin binders; Chemistry (all)
Elenco autori:
E. Bonandi, F. Foschi, C. Marucci, F. Dapiaggi, M. Sironi, S. Pieraccini, M.S. Christodoulou, F. de Asís Balaguer, J.F. Díaz, N. Zidar, D. Passarella
Link alla scheda completa: