521087-25-2Relevant academic research and scientific papers
Synthesis of novel 2-O,3′-N-linked macrocyclic taxoids with variable ring size
Querolle, Olivier,Dubois, Joelle,Thoret, Sylviane,Dupont, Christophe,Gueritte, Francoise,Guenard, Daniel
, p. 542 - 550 (2007/10/03)
A series of macrocyclic taxoids was prepared by connecting the 2-OH and 3′-NH moieties with aliphatic chains to mimic the docetaxel solid-state conformation. The synthesis was achieved by acylation of both positions with various bromoalkanoic acids, and ring closure was carried out with sodium sulfide. Nine 19- to 27-membered macrocyclic taxoids were obtained and evaluated as inhibitors of microtubule disassembly as well as for their cytoxicity. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003.
