Tubulin-guided dynamic combinatorial library of thiocolchicine-podophyllotoxin conjugates

G Cappelletti; D Cartelli; B Peretto; M Ventura; M Riccioli; F Colombo; John Snaith; S Borrelli; D Passarella

doi:10.1016/j.tet.2011.07.038

Tubulin-guided dynamic combinatorial library of thiocolchicine-podophyllotoxin conjugates

G Cappelletti, D Cartelli, B Peretto, M Ventura, M Riccioli, F Colombo, John Snaith, S Borrelli, D Passarella

Chemistry

Research output: Contribution to journal › Article

16 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	7354-7357
Number of pages	4
Journal	Tetrahedron
Volume	67
Issue number	38
DOIs	https://doi.org/10.1016/j.tet.2011.07.038
Publication status	Published - 1 Sept 2011

Keywords

Dynamic combinatorial chemistry
Target-guided synthesis
Disulfide-exchange reaction

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10.1016/j.tet.2011.07.038

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title = "Tubulin-guided dynamic combinatorial library of thiocolchicine-podophyllotoxin conjugates",

abstract = "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.",

keywords = "Dynamic combinatorial chemistry, Target-guided synthesis, Disulfide-exchange reaction",

author = "G Cappelletti and D Cartelli and B Peretto and M Ventura and M Riccioli and F Colombo and John Snaith and S Borrelli and D Passarella",

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doi = "10.1016/j.tet.2011.07.038",

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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

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 -

Tubulin-guided dynamic combinatorial library of thiocolchicine-podophyllotoxin conjugates

Abstract

Keywords

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