Cancer-targeted therapy is an expanding and successful approach in treatment of many types of cancers. One of the main categories of targeted therapy is use of small molecule inhibitors. 15-Lipoxygenase (15-LOX) is an enzyme which reacts with polyunsaturated fatty acids and produces metabolites that are implicated in many important human diseases, such as cancer. Considering the role of 15-LOX (mainly 15-LOX-1) in the progression of some cancers, the discovery of 15-LOX inhibitors could potentially lead to development of novel cancer therapeutics and it can be claimed that 15-LOX inhibitors might be suitable as chemotherapy agents in the near future. This article reviews relevant publications on 15-LOX inhibitors with focus on their anticancer activities in vitro and in vivo. Many 15-LOX inhibitors have been reported for which separate studies have shown their anticancer activities. This review paves the way to further explore the mechanism of their antiproliferative effects via 15-LOX inhibition.
In this study, we report the design, synthesis, and structure-activity relationships of a series of 5-amido-1-(2,4-dinitrophenyl)-1H-4-pyrazolecarbonitriles as DD-carboxypeptidase/penicillin-binding protein (PBP) inhibitors with Grampositive antibacterial activity. Our results show that the compounds with larger, more polarizable, and electron-rich substituted benzamide moieties such as paradimethyaminobenzamide (3j) and para-methoxybenzamide (3i) exhibit better antibacterial activity against methicillin-susceptible Staphylococcus aureus and methicillin-resistant Staphylococcus aureus with minimum inhibition concentration (MIC) values of 3.8 and 15.3 lM for both of them. These results are in accordance MEDICINAL CHEMISTRY RESEARCH with estimated inhibition constants (K i ) that are obtained from docking with PBP2 and PBP4 of Staphylococcus aureus.
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