Affiliation:
1. Department of Chemistry, N. I. Lobachevsky State University of Nizhny Novgorod
2. Laboratory of Cell Interactions, Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry RAS
Abstract
An efficient seven-step semisynthetic approach towards non-racemic bifunctional furano-allocolchicinoids, starting from naturally occurring colchicine is presented. The Pd-catalyzed domino Sonogashira coupling/5-endo-dig cyclization was employed as the key step. The prepared compounds exhibited substantial cytotoxicity against T3M4, MiaPaCa-2, Colo-357, and PANC-1 cell lines. The presence of two functionalities with different reactivity (hydroxyl and amino groups) in the target molecules allows for an easy conjugation of furano-allocolchicinoids with drug delivery carriers, and opens promising opportunities for their further exploitation in the search of therapeutics.
Funder
Russian Science Foundation
Subject
Organic Chemistry,Catalysis
Cited by
8 articles.
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