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Synthesis and Biological Evaluation of Novel Carbohydrate‐Derived Derivatives of Erlotinib
Author(s) -
Yu Wenbo,
Jiang Luxia,
Shen Chao,
Zhang Pengfei
Publication year - 2016
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.21328
Subject(s) - erlotinib , chemistry , carbohydrate , in vitro , pharmacology , erlotinib hydrochloride , a549 cell , cycloaddition , biochemistry , epidermal growth factor receptor , catalysis , biology , receptor
Preclinical ResearchA 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.