TY - JOUR
T1 - Tubulin-guided dynamic combinatorial library of thiocolchicine-podophyllotoxin conjugates
AU - Cappelletti, G
AU - Cartelli, D
AU - Peretto, B
AU - Ventura, M
AU - Riccioli, M
AU - Colombo, F
AU - Snaith, John
AU - Borrelli, S
AU - Passarella, D
PY - 2011/9/1
Y1 - 2011/9/1
N2 - The use of tubulin as a target to influence the composition of the mixture from a dynamic combinatorial library, based on the disulfide bond exchange reaction, is described. ESI-FT-ICR-MS was used to determine the composition of the library. The heterodimeric compound amplified by this approach was used to design the homologous derivative with a two-carbon spacer in place of the disulfide function. The ability of the compounds to inhibit tubulin polymerization is reported and compared to thiocolchicine. (C) 2011 Elsevier Ltd. All rights reserved.
AB - The use of tubulin as a target to influence the composition of the mixture from a dynamic combinatorial library, based on the disulfide bond exchange reaction, is described. ESI-FT-ICR-MS was used to determine the composition of the library. The heterodimeric compound amplified by this approach was used to design the homologous derivative with a two-carbon spacer in place of the disulfide function. The ability of the compounds to inhibit tubulin polymerization is reported and compared to thiocolchicine. (C) 2011 Elsevier Ltd. All rights reserved.
KW - Dynamic combinatorial chemistry
KW - Target-guided synthesis
KW - Disulfide-exchange reaction
UR - https://www.scopus.com/pages/publications/80051781198
U2 - 10.1016/j.tet.2011.07.038
DO - 10.1016/j.tet.2011.07.038
M3 - Article
VL - 67
SP - 7354
EP - 7357
JO - Tetrahedron
JF - Tetrahedron
IS - 38
ER -