title: Synthesis and Biological Evaluation of Novel Carbohydrate-Derived Derivatives of Erlotinib.
abstract: Preclinical Research 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.
authors: College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou, 310014, China.|Linjiang College, Hangzhou Vocational and Technical College, Hangzhou, 310018, China.
authors: Wenbo
authors: W
authors: Yu
authors: College of Material, Chemistry and Chemical Engineering, Hangzhou Normal University, Hangzhou, 310016, China.
authors: Luxia
authors: L
authors: Jiang
authors: College of Material, Chemistry and Chemical Engineering, Hangzhou Normal University, Hangzhou, 310016, China.
authors: Chao
authors: C
authors: Shen
authors: College of Material, Chemistry and Chemical Engineering, Hangzhou Normal University, Hangzhou, 310016, China.
authors: Pengfei
authors: P
authors: Zhang
mesh_terms: D000072283:A549 Cells; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002241:Carbohydrates / Q000737:chemistry; D045744:Cell Line, Tumor; D000069347:Erlotinib Hydrochloride / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D061986:MCF-7 Cells; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D002241:Carbohydrates; D000069347:Erlotinib Hydrochloride
keywords: antitumor activity; erlotinib; glycoconjugates