Title

Chlorophyll-a derivatives in photodynamic therapy: Effect of position of heptyl ether side-chains on in vivo photosensitizing activity

Document Type

Article

Publication Date

1-9-1996

Abstract

Syntheses and comparative in vivo photosensitizing efficacy of a series of chlorophyll-a derivatives with (1-heptyloxyethyl) substituents at various positions are discussed. Compared with Photofrin®, the n-heptyl ether analogues showed better in vivo sensitizing activity (DBA/2 mice transplanted with SMT/F tumors) as well as reduced skin phototoxicity. The Vilsmeier formylation of copper(II) methyl mesopyropheophorbide-a 11 did not produce the expected meso-formyl derivative 12, but instead gave the α,β-unsaturated chloroformyl analogue 13 as the major product.

Publication Source (Journal or Book title)

Bioorganic and Medicinal Chemistry Letters

First Page

105

Last Page

110

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