Design, Synthesis And Evaluation Of Adss Bisubstrate Inhibitors
CHEMMEDCHEM(2020)
Abstract
Many cancers lack the expression of methylthioadenosine phosphorylase (MTAP). These cancers require adenylosuccinate synthetase (AdSS) for nucleic acid synthesis. By inhibiting adenylosuccinate synthetase, we potentially have a new therapeutic agent. Bisubstrate inhibitors were synthesized and evaluated against purified AdSS. The best activity was obtained with adenosine bearing a four-carbon linker that connects theN-formyl-N-hydroxy moiety to the 6-position of the purine nucleoside.
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Key words
adenylosuccinate synthetase, lung cancer, methylthioadenosine phosphorylase, small molecules
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