title: Synthesis and biological assay of erlotinib analogues and BSA-conjugated erlotinib analogue.
abstract: A series of erlotinib analogues that have structural modification at 6,7-alkoxyl positions is efficiently synthesized. The in vitro anti-tumor activity of synthesized compounds is studied in two non-small cell lung cancer (NSCLC) cell lines (A549 and H1975). Among the synthesized compounds, the iodo compound 6 (ETN-6) exhibits higher anti-cancer activity compared to erlotinib. An efficient method is developed for the conjugation of erlotinib analogue-4, alcohol compound, with protein, bovine serum albumin (BSA), via succinic acid linker. The in vitro anti-tumor activity of the protein attached erlotinib analogue, 8 (ETN-4-Suc-BSA), showed stronger inhibitory activity in both A549 and H1975 NSCLC cell lines.
authors.affiliation: Department of Chemistry, National Dong Hwa University, Soufeng, Hualien 974, Taiwan; Department of Nursing, Tzu Chi University of Science and Technology, Hualien 970, Taiwan.
authors.forename: Ramalingam
authors.initials: R
authors.lastname: Boobalan
authors.affiliation: Department of Biological Science and Technology, National Chiao Tung University, Hsinchu 30068, Taiwan.
authors.forename: Kuang-Kai
authors.initials: KK
authors.lastname: Liu
authors.affiliation: Department of Biological Science and Technology, National Chiao Tung University, Hsinchu 30068, Taiwan. Electronic address: jichao@faculty.nctu.edu.tw.
authors.forename: Jui-I
authors.initials: JI
authors.lastname: Chao
authors.affiliation: Department of Chemistry, National Dong Hwa University, Soufeng, Hualien 974, Taiwan; Department of Nursing, Tzu Chi University of Science and Technology, Hualien 970, Taiwan. Electronic address: chinpiao@mail.ndhu.edu.tw.
authors.forename: Chinpiao
authors.initials: C
authors.lastname: Chen
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy* / Q000473:pathology; D002417:Cattle; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D000069347:Erlotinib Hydrochloride / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D008168:Lung / Q000187:drug effects / Q000473:pathology; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000473:pathology; D008958:Models, Molecular; D012710:Serum Albumin, Bovine / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D012710:Serum Albumin, Bovine; D000069347:Erlotinib Hydrochloride
keywords: Anti-cancer; BSA; EGFR; Erlotinib; NSCLC