The photosensitizing and pharmacokinetic properties of porphyrin-type compounds have been investigated for nearly a century. In the last decade, two porphyrin derivatives were approved in the U.S.A. and in several other countries for the photodynamic treatment of various lesions. An overview of the different mechanisms for preferential porphyrinoid localization in malignant tumors is presented herein. Several uptake pathways are possible for each photosensitizer, which are determined by its structure, mode of delivery and tumor type. Comparisons of the different mechanisms and correlations with the structure of the sensitizer are presented. Current delivery systems for porphyrin sensitizers are described, as well as recent strategies for enhancing their tumor-specificity, including conjugation to a carrier system that selectively targets a tumor-associated receptor or antigen.

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The literature on the synthesis and the biological properties of boron-containing chlorins and phthalocyanines is reviewed. A series of homologous derivatives of pyropheophorbide A is described. The compounds contain the B(12)H(11)SH(2-) cluster attached to the single carboxyl group and vary in the length of the alkyl chain (methyl, propyl, pentyl, heptyl and nonyl) attached via an ether linkage to the former vinyl group. Cellular uptake was found for all derivatives except the nonyl sidechain. The compounds were moderately cell-toxic. Localization in lysosomes could be excluded; the compounds localized probably in the mitochondria.

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Organic chemistry Z 0200 Boron-Containing Chlorins and Tetraazaporphyrins: Synthesis and Cell Uptake of Boronated Pyropheophorbide A Derivatives -[26 refs.]. -(RATAJSKI, M.; OSTERLOH, J.; GABEL, D.; Anti-Cancer Agents Med. Chem. 6 (2006) 2, 159-166; Fachbereich Chem., Univ. Bremen, D-28334 Bremen, Germany; Eng.) -Lindner 44-230