Design,Synthesis and Pharmacological Evaluation of Noscapine Glycoconjugates

摘要

The present work is directed to design a series of molecules which are hybrids of two non-toxic biocompatible chemical architectures,noscapine and carbohydrates.Fourteen,7-Onoscapine analogues have been synthesized out of which one of the analogue is 7-O-propargylated derivative and others are in its glycoconjugate form with triazole bridging achieved via Click reaction,where dinuclear copper(I)thiodiacetate complex [(PPh3)2Cu(μ-tda)Cu(PPh3)2].6H2O has been emerged as an excellent catalyst for the noscapine-glyco Click-coupling.All the developed noscapine glycoconjugates have been investigated for anticancer activity using HeLa cell line and antileishmanial activity against Leishmania donovani.Result indicates that five of the developed noscapine glycoconjugates(5a,5b,5c,5e and 5l)showed significant anti-proliferative activity.On the other hand,four of them(5b,5c,5e,and 5l)showed significant anti-leishmanial activity.