Topoisomerases I and II play a crucial role in biological processes involving DNA. One such process is replication of DNA during cell division thus, making them a target for anti-cancer drugs. Currently camptothecin derivatives (Topotecan & Irinotecan) are the only approved anti-cancer drugs that inhibit Topo I. Due to their chemical instability in basic pH (i.e. lactone ring opening) there is still ongoing research in search for better Topo I poisons. Luotonin,quinazolinone containing natural product, offers better chemical stability however with reduced levels of Topo I inhibition activity. So, there have been efforts aimed at improving its Topo-I inhibition levels by structural modifications. Though there are several reports on substituted Luotonins the C-ring aromatic substitution is still not known thus, in our research we have initiated efforts in accessing alibrary with C-ring aromatic substitutions of Luotonin through a key Intra Molecular Aza-Michael reaction (IMAMR) of quinazolinonyl chalcones. Their synthesis and  and Topo-I inhibition activity assay results  will be presented.<br/>

Facile access to C-ring aromatic substituted luotonins and vasicinones for Topo I inhibition via intramolecular aza-Michael reactions (IMAMRs) of quinazolinonyl chalcones

2019 Fall National Meeting

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