Methyl pyropheophorbide-a analogues: Potential fluorescent probes for the peripheral-type benzodiazepine receptor. Effect of central metal in photosensitizing efficacy

作者:Chen Y; Zheng X; Dobhal MP; Gryshuk A; Morgan J; Dougherty TJ; Oseroff A; Pandey RK*
来源:Journal of Medicinal Chemistry, 2005, 48(11): 3692-3695.
DOI:10.1021/jm050039k

摘要

Pyropheophorbides and their metal complexes were synthesized to investigate their applications as nonradioactive peripheral benzodiazepine receptor (PBR) binding probes and photosensitizers for use in photodynamic therapy. They were found to be localized in mitochondria and showed significant binding to PBR. In some cases, the PBR binding values were similar to that for 17 (PK11195, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)isoquinoline-3-carboxamide). However, no direct correlation between 17 displacement ability and photosensitizing efficacy of photosensitizers was observed.

  • 出版日期2005-6-2