Coumarin and Stilbenes derivatives structurally related as DNA polymerase inhibitors

PERRETI M; BRUNA-HAUPT, EZEQUIEL; CELINA GARCÍA; CARRILLO R; H.A. GARRO; C. R. PUNGITORE

Simposio; RSEQ Symposium 2021; 2021

Possibly, the earliest enzyme activity to appear in evolution was the ability to accurately replicate the genome, which is a prerequisite for evolution itself. DNA polymerases govern the cell cycle and participate in the synthesis of genetic material. Therefore, the inhibition of these enzymes would lead to cell death, so the substances capable of producing said inhibition would be potential anticancer agents.[1] Coumarins and stilbenes (Scheme 1) are low molecular weight compounds with no adverse side effects or toxicity, allowing these and other properties to make them potential drug candidates against many diseases.[2], [3] For this reason, an interesting number of organic derivates obtained by chemical synthesis and chemical modifications of coumarins and scaffold stilbenes were tested on Taq DNA polymerase (Fig. 1) in PCR assays in order to evaluate their antiproliferative activity.