CHLOROPHYLL-A DERIVATIVES IN PHOTODYNAMIC THERAPY - EFFECT OF POSITION OF HEPTYL ETHER SIDE-CHAINS ON IN-VIVO PHOTOSENSITIZING ACTIVITY

Authors
PANDEY RK CONSTANTINE S GOFF DA KOZYREV AN DOUGHERTY TJ SMITH KM
Citation
Rk. Pandey et al., CHLOROPHYLL-A DERIVATIVES IN PHOTODYNAMIC THERAPY - EFFECT OF POSITION OF HEPTYL ETHER SIDE-CHAINS ON IN-VIVO PHOTOSENSITIZING ACTIVITY, Bioorganic & medicinal chemistry letters, 6(1), 1996, pp. 105-110
Citations number
21
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
1
Year of publication
1996
Pages
105 - 110
Database
ISI
SICI code
0960-894X(1996)6:1<105:CDIPT->2.0.ZU;2-7
Abstract
Syntheses and comparative in vivo photosensitizing efficacy of a serie s of chlorophyll-a derivatives with (1-heptyloxyethyl) substituents at various positions are discussed. Compared with Photofrin (R), the n-h eptyl ether analogues showed better in vivo sensitizing activity (DBA/ 2 mice transplanted with SMT/F tumors) as well as reduced skin phototo xicity. The Vilsmeier formylation of copper(II) methyl mesopyropheopho rbide-a 11 did not produce the expected meso-formyl derivative 12, but instead gave the alpha,beta-unsaturated chloroformyl analogue 13 as t he major product.