Evaluation of analogues of furan-amidines as inhibitors of NQO2
Bioorganic & Medicinal Chemistry Letters, ISSN: 0960-894X, Vol: 28, Issue: 8, Page: 1292-1297
2018
- 17Citations
- 34Captures
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Metrics Details
- Citations17
- Citation Indexes17
- 17
- CrossRef12
- Captures34
- Readers34
- 34
Article Description
Inhibitors of the enzyme NQO2 (NRH: quinone oxidoreductase 2) are of potential use in cancer chemotherapy and malaria. We have previously reported that non-symmetrical furan amidines are potent inhibitors of NQO2 and here novel analogues are evaluated. The furan ring has been changed to other heterocycles (imidazole, N -methylimidazole, oxazole, thiophene) and the amidine group has been replaced with imidate, reversed amidine, N -arylamide and amidoxime to probe NQO2 activity, improve solubility and decrease basicity of the lead furan amidine. All compounds were fully characterised spectroscopically and the structure of the unexpected product N -hydroxy-4-(5-methyl-4-phenylfuran-2-yl)benzamidine was established by X-ray crystallography. The analogues were evaluated for inhibition of NQO2, which showed lower activity than the lead furan amidine. The observed structure-activity relationship for the furan-amidine series with NQO2 was rationalized by preliminary molecular docking and binding mode analysis. In addition, the oxazole-amidine analogue inhibited the growth of Plasmodium falciparum with an IC 50 value of 0.3 μM.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0960894X1830204X; http://dx.doi.org/10.1016/j.bmcl.2018.03.025; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85044107050&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/29567345; https://linkinghub.elsevier.com/retrieve/pii/S0960894X1830204X; https://dx.doi.org/10.1016/j.bmcl.2018.03.025
Elsevier BV
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