University of Texas System

Other

Pro-neuron, Inc.

Wallace Technologies

Abdallah Cherif

David Farquhar

David J Yang

Sidney Wallace

Anthracycline analogues bearing latent alkylating substituents

The present invention is a compound having the structure

Methods of treatment with anthracycline derivatives

The present invention involves a rapid synthesis of .sup.18 F-FMISO and analogs thereof. New precursors such as 1-(2'-nitro-1'-imidazolyl)-2-0-acetyl-3-0-tosylpropanol, glycerol-1,3-ditosylate-2-0-acetylate, 1-(2'-nitro-1'-imidazolyl)-2,3-0-diacetyl-4-0-tosylbutanol and threitol 1,4-di-tosylate-2,3-0-diacetylate, are also important aspects of the invention. A further aspect of the invention is the development of a hydrophilic PET ligand to image tumor hypoxia. Erythrotosyl analogue of 2-nitroimidazone (Ts-ETNIM) was prepared from a mixture of 2-nitromidazole, ditosylthreitol and cesium carbonate at 60.degree. C. for 1 hr. Ts-ETNIM was isolated at 70% yield. �.sup.18 F!fluoroerythronitroimidazole (FETNIM) was then prepared from Ts-ETNIM and K.sup.18 F/kryptofix.RTM.. The yield for �.sup.18 F!FETNIM was 26-30% (60 min, decay corrected). Results of biodistribution and PET studies indicate that �.sup.18 F!FETNIM has the potential to detect tumor hypoxia and is indicated to be less neurotoxic.

Rapid synthesis and use of 18F-fluoromisonidazole and analogs

(2'-nitro-1'-imidazolyl)-2,3-isopropylidene-y-tosylbutanol, a precursor

The present invention is a compound having the structure ##STR1##

Growing community of inventors

Houston, TX, United States of America

Abdallah Cherif