In order to evaluate structure-activity relationships in the benzochlorin ring system, a series of functionalized benzochlorins have been synthesized by modifying the sulfonic acid group of octaethylbenzochlorin sulfonic acid (OEBCS). Using very simple chemistry it has been possible to produce a large number of benzochlorins that differ only in the nature of functionality of a pendant side arm. The introduction of zinc or tin into the benzochlorin macrocycle produces the corresponding metallated benzochlorins that retain the original functionality. The synthesis and spectroscopic properties of the free base and metallobenzochlorins are discussed. Preliminary in vivo results show that different functionality causes significant differences in biological efficacy.

Date Published: 2 April 1996
PDF: 12 pages
Proc. SPIE 2675, Optical Methods for Tumor Treatment and Detection: Mechanisms and Techniques in Photodynamic Therapy V, (2 April 1996); doi: 10.1117/12.237537

Published in SPIE Proceedings Vol. 2675:
Optical Methods for Tumor Treatment and Detection: Mechanisms and Techniques in Photodynamic Therapy V
Thomas J. Dougherty, Editor(s)