Abstract
Recent publications highlighted that vinca derivatives either functionalized on C-12' or enlarged on cycle C' could be more cytotoxic than vinblastine or vinorelbine, both used in anti-cancer therapy. By combining these two results, nine new 7'-homo-anhydrovinblastine derivatives functionalized on C-13' were elaborated. The synthesis of key intermediates, their one-step transformation into final products in mild conditions and their biological activities are presented.
Keywords:
7′-homo-Anhydrovinblastine; Cancer; Cytotoxicity; Tubulin; Vinca alkaloids.
Copyright © 2015 Elsevier Ltd. All rights reserved.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Antineoplastic Agents / chemical synthesis*
-
Antineoplastic Agents / chemistry
-
Antineoplastic Agents / pharmacology
-
Cell Line, Tumor
-
Cell Proliferation / drug effects
-
HCT116 Cells
-
Humans
-
K562 Cells
-
Tubulin / chemistry
-
Tubulin / metabolism
-
Tubulin Modulators / chemical synthesis
-
Tubulin Modulators / chemistry
-
Tubulin Modulators / pharmacology
-
Vinblastine / analogs & derivatives*
-
Vinblastine / chemical synthesis
-
Vinblastine / chemistry
-
Vinblastine / pharmacology
-
Vinca Alkaloids / chemistry
-
Vinorelbine
Substances
-
Antineoplastic Agents
-
Tubulin
-
Tubulin Modulators
-
Vinca Alkaloids
-
Vinblastine
-
Vinorelbine