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1. (WO2001085736) PORPHYRIN-BASED NEUTRON CAPTURE AGENTS FOR CANCER THERAPY

Pub. No.:    WO/2001/085736    International Application No.:    PCT/US2001/015433
Publication Date: Nov 15, 2001 International Filing Date: May 9, 2001
IPC: A61K 41/00
C07D 487/22
C07F 5/05
Applicants: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
VICENTE, M., G., H.
SHETTY, S., J.
JAQUINOD, L.
SMITH, K., M.
Inventors: VICENTE, M., G., H.
SHETTY, S., J.
JAQUINOD, L.
SMITH, K., M.
Title: PORPHYRIN-BASED NEUTRON CAPTURE AGENTS FOR CANCER THERAPY
Abstract:
The invention describes the synthesis of a panel of novel carbon-carbon linked carboranyl-containing 5,10,15,20-tetraphenylporphyrins bearing 25-44 % boron by weight. Preliminary in vitro evaluation of several of these compounds, using both rat and human brain tumor cell lines, shows that these compounds display very low cytotoxicities, are capable of delivering substantial amounts of boron intracellularly, and are retained for long periods of time.