Skok, Z; Durcik, M; Skledar, DG; Barancokova, M; Masic, LP; Tomasic, T; Zega, A; Kikelj, D; Zidar, N; Ilas, J in [Skok, Ziga; Durcik, Martina; Skledar, Darja Gramec; Barancokova, Michaela; Masic, Lucija Peterlin; Tomasic, Tihomir; Zega, Anamarija; Kikelj, Danijel; Zidar, Nace; Ilas, Janez] Univ Ljubljana, Fac Pharm, Askerceva Cesta 7, Ljubljana 1000, Slovenia published Discovery of new ATP-competitive inhibitors of human DNA topoisomerase II alpha through screening of bacterial topoisomerase inhibitors in 2020.0, Cited 50.0. Name: 4-Nitrobenzoic acid. The Name is 4-Nitrobenzoic acid. Through research, I have a further understanding and discovery of 62-23-7.
Human DNA topoisomerase II is one of the major targets in anticancer therapy, however ATP-competitive inhibitors of this target have not yet reached their full potential. ATPase domain of human DNA topoisomerase II belongs to the GHKL ATPase superfamily and shares a very high 3D structural similarity with other superfamily members, including bacterial topoisomerases. In this work we report the discovery of a new chemotype of ATP-competitive inhibitors of human DNA topoisomerase II alpha that were discovered through screening of in-house library of ATP-competitive inhibitors of bacterial DNA gyrase and topoisomerase IV. Systematic screening of this library provided us with 20 hit compounds. 1,2,4-Substituted N-phenylpyrrolamides were selected for a further exploration which resulted in 13 new analogues, including 52 with potent activity in relaxation assay (IC50 = 3.2 mu M) and ATPase assay (IC50 = 0.43 mu M). Cytotoxic activity of all hits was determined in MCF-7 cancer cell line and the most potent compounds, 16 and 20, showed an IC50 value of 8.7 and 8.2 mu M, respectively.
Name: 4-Nitrobenzoic acid. About 4-Nitrobenzoic acid, If you have any questions, you can contact Skok, Z; Durcik, M; Skledar, DG; Barancokova, M; Masic, LP; Tomasic, T; Zega, A; Kikelj, D; Zidar, N; Ilas, J or concate me.
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