Abstract
Professor Ross of London University, England, was using nitrogen mustard to treat cancers by attacking both strands of tumor DNA. As a part of my doctoral thesis, I am to design drugs using aziridine to attack only one strand of DNA. Over the years, I made over 100 dinitrophenyl aziridine derivatives. One of them is dinitrobenzamide (CB1954) which gives a CI of 70, highest toxicity to animal tumor ever recorded. CB1954 wipes out a solid aggressive tumor by attacking a single-strand DNA of Walker carcinoma 256, in rat. My greatest challenge at NCI in USA is to translate the animal work which I did in London University to humans. As radiolabeled methylated quinone crosses the blood-brain barrier in mice, I decided to use quinone moiety as a carrier for aziridine rings to attack glioblastomas, the brain tumor in humans. By attaching two aziridines and two carbamate moieties to quinone, I made AZQ (US Patent 4,146,622). By treating brain cancer with AZQ , we observed that glioblastoma tumor not only stops growing but also starts shrinking. Literature search showed that AZQ is extensively studied.