2. Academic Validation
  3. Syntheses of new chlorin derivatives containing maleimide functional group and their photodynamic activity evaluation

Syntheses of new chlorin derivatives containing maleimide functional group and their photodynamic activity evaluation

  • Bioorg Med Chem Lett. 2015 Oct 1;25(19):4078-81. doi: 10.1016/j.bmcl.2015.08.036.
Xiuhan Guo 1,  Liu Wang 1,  Shisheng Wang 2,  Yueqing Li 1,  Fan Zhang 1,  Bo Song 3,  Weijie Zhao 4
Affiliations

Affiliations

  • 1 School of Pharmaceutical Science and Technology, State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024, PR China.
  • 2 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.
  • 3 School of Chemistry, Dalian University of Technology, Dalian 116024, PR China.
  • 4 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.
PMID: 26306981 DOI: 10.1016/j.bmcl.2015.08.036
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.

Keywords

Chlorin derivatives; Chlorin e6; Photo cytotoxic activity; Singlet oxygen.

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