Synthesis of Analogues of NSC73306 to Circumvent Multidrug Resistance in Cancer

National Heart, Lung, And Blood Institute

Investigators

Linked publications, trials & patents

Abstract

More recently with the help of a summer student (Jiayang Li), I have synthesized an additional twenty-three compounds based on our experiences with the first set and the commercial availability of intermediates. The p-dimethylamino substituted derivative was finally prepared after much labor and, as expected, found to be soluble in dilute acid, but as the sample was diluted even further for testing, precipitation occurred due to its weak basicity. Therefore a new synthesis involving the much more strongly basic p-dimethylaminomethyl derivative was developed and its synthesis is nearing completion. I also continue to examine the structures of related proteins in the GFP series by digestion and LC/MS (J.-R. Gillet). The synthesized compounds are being tested for its selectivity in killing cancer cells. In particular, cancel cells that are showing multidrug-resistance.