title: Syntheses of new chlorin derivatives containing maleimide functional group and their photodynamic activity evaluation.
abstract: Nine new chlorin derivatives containing maleimide functional group and amino acid residue with chlorin e6 scaffold (compounds 1-6) or pheophorbide a scaffold (compounds 7-9) were synthesised from chlorophyll a. The all nine derivatives demonstrated increased photo cytotoxic activity in HepG2 cell (IC50 3.2-20.5 μM) comparing with chlorin e6 and its trimethyl ester. Their photo cytotoxicities were approximately dependent on their abilities to produce singlet oxygen ((1)O2) in the cells.
authors: School of Pharmaceutical Science and Technology, State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024, PR China.
authors: Xiuhan
authors: X
authors: Guo
authors: School of Pharmaceutical Science and Technology, State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024, PR China.
authors: Liu
authors: L
authors: Wang
authors: School of Pharmaceutical Science and Technology, State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024, PR China. Electronic address: wangss@dlut.edu.cn.
authors: Shisheng
authors: S
authors: Wang
authors: School of Pharmaceutical Science and Technology, State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024, PR China.
authors: Yueqing
authors: Y
authors: Li
authors: School of Pharmaceutical Science and Technology, State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024, PR China.
authors: Fan
authors: F
authors: Zhang
authors: School of Chemistry, Dalian University of Technology, Dalian 116024, PR China.
authors: Bo
authors: B
authors: Song
authors: School of Pharmaceutical Science and Technology, State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024, PR China. Electronic address: zyzhao@dlut.edu.cn.
authors: Weijie
authors: W
authors: Zhao
mesh_terms: D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D056945:Hep G2 Cells; D006801:Humans; D008301:Maleimides / Q000737:chemistry* / Q000494:pharmacology*; D008968:Molecular Conformation; D017319:Photosensitizing Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011166:Porphyrins / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D008301:Maleimides; D017319:Photosensitizing Agents; D011166:Porphyrins; C043592:maleimide; C006969:chlorin
keywords: Chlorin derivatives; Chlorin e6; Photo cytotoxic activity; Singlet oxygen