Synthesis and Biological Evaluation of Novel Carbohydrate ‐Derived Derivatives of Erlotinib

Abstract A series of novel carbohydrate‐derived Erlotinib derivatives were prepared by the copper‐catalyzed cycloaddition reaction of erlotinib with various azido‐sugars. The structures of the newly synthesized compounds were characterized and their cytostatic effects evaluated in vitro on human cancer cell lines MDA‐MB‐231, HEPG‐2, A549, and MCF‐7 using an MTS assay. The novel erlotinib derivatives had the expected inhibitory effects on MDA‐MB‐231 and HEPG‐2 cell llines. Among the compounds evaluated the carbohydrate‐derived compounds 5b, 5d, 6a, and 6c had more potent activities against MDA‐MB‐231 or HEPG‐2 than Erlotinib. Drug Dev Res, 2016. © 2016 Wiley Periodicals, Inc.
Source: Drug Development Research - Category: Drugs & Pharmacology Authors: Tags: Research Article Source Type: research