Compounds with activity on Taq DNA polymerase

EZEQUIEL BRUNA-HAUPT; CARLOS R. PUNGITORE; MARCELLE D. PERRETTI; ROMEN CARRILLO; TANAUSÚ SANTOS

La Laguna, Tenerife

Congreso; COST Action CM1407; 2018

COST

DNA polymerases are enzymes that participate in the cell cycle and are involved in the synthesis of genetic material, in addition to transferring genetic information correctly in the processes of cell division. Therefore, the inhibition of these enzymes would lead to cell death, so that substances capable of producing such inhibition would be potential anticancer agents.Taq polymerase is a type of thermostable DNA polymerase that is produced by the bacterium Thermus aquaticus (T-aq) and from which it was isolated by Thomas D. Brock in 1968 (Figure 1). This enzyme has a close evolutionary relationship with human DNA polymerases [1]; In addition, it is known for its thermostability and for its application in polymerization chain reactions (PCR).Coumarins are secondary metabolites of plants that show a lot of pharmacological properties [2], and have been studied intensively in the search for new drugs with diverse activities. Therefore, synthesize derivatives of these structures and measure their potential antitumor activity, has high interest, in order to establish a structure activity relationship much more precise and thus, obtain compounds with possible pharmacological activity [3].References:[1] Pungitore C.R. (2014). Current Enzyme Inhibition 10: 13-38.[2] Garro H.A., García C., Martín V.S., Tonn C.E., Pungitore C.R. (2015). Bioorg. Med. Chem. Lett. 25: 914-918.[3] Bruna-Haupt E., Garro H.A., Gutiérrez L., Pungitore C.R. (2018). Med. Chem. Research 27: 1432-1442.