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Identification of NQO1 and ferrochelatase as interaction partners for neuroprotective N‐{[2‐(4‐phenyl‐piperazin‐1‐yl)‐ethyl]‐phenyl}‐arylamides
10.1111/cbdd.13193 2018-04-10 Affinity chromatography was used to identify potential cellular targets that are responsible for neuroprotective activity of N‐{[2‐(4‐phenyl‐piperazin‐1‐yl)‐ethyl]‐phenyl}‐arylamides. Active and inactive representatives of N‐{[2‐(4‐phenyl‐piperazin‐1‐yl)‐ethy... |
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Identification of inhibitors of Tartrate‐resistant acid phosphatase (TRAP/ACP5) activity by small‐molecule screening
10.1111/cbdd.13187 2018-03-30 Tartrate‐resistant acid phosphatase (TRAP/ACP5) occurs as two isoforms—TRAP 5a with low enzymatic activity due to a loop interacting with the active site and the more active TRAP isoform 5b generated upon proteolytic cleavage of this loop. TRAP has been impli... |
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Antinociceptive potency of enkephalins and enkephalinase inhibitors in the mouse model of colorectal distension—proof‐of‐concept
10.1111/cbdd.13186 2018-03-30 Irritable bowel syndrome (IBS) is a chronic disease characterized by abdominal pain and changes in bowel habits. Patients with IBS comprise a significant portion of attendants at the outpatient clinics. Targeting intestinal opioid receptors was found successf... |
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Bis‐2(5H)‐furanone derivatives as new anticancer agents: Design, synthesis, biological evaluation, and mechanism studies
10.1111/cbdd.13183 2018-03-25 New bis‐2(5H)‐furanone derivatives containing a benzidine core were synthesized via a one‐step transition‐metal‐free reaction of benzidine with 5‐substituted 3,4‐dihalo‐2(5H)‐furanones. Their antitumor activities against various tumor cells have been evaluate... |
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New thiophene–acridine compounds: Synthesis, antileishmanial activity, DNA binding, chemometric, and molecular docking studies
10.1111/cbdd.13176 2018-03-25 In this study, we synthesized eight new compounds containing the 2‐amino‐cycloalkyl[b]thiophene and acridine moieties (ACT01 and ACS01‐ACS07). None tested compounds presented human erythrocyte cytotoxicity. The new compounds presented antipromastigote activit... |
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Design, synthesis and evaluation of genipin derivatives for the treatment of Alzheimer's Disease
10.1111/cbdd.13194 2018-03-15 Twenty two novel genipin derivatives have been designed, synthesized and evaluated for their inhibitory activity against acetylcholinesterase (AChE). As a result, compound 13a bearing ligustrazine moiety displayed the most potent AChE inhibitory activity in t... |
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1,2,3,4‐Tetrahydroisoquinolines as inhibitors of HIV‐1 integrase and human LEDGF/p75 interaction
10.1111/cbdd.13175 2018-03-15 Alkaloids are a class of organic compounds with a wide range of biological properties, including anti‐HIV activity. The 1,2,3,4‐tetrahydroisoquinoline is a ubiquitous structural motif of many alkaloids. Using a short and an efficient route for synthesis, a se... |
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Cover Image
10.1111/cbdd.13190 2018-03-14 The cover image, by Sophie L. Dahl et al., is based on the Research Article Interaction of antivirals with a heptameric bundle model of the p7 protein of hepatitis C virus, DOI: 10.1111/cbdd.13162. |
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Rational design of isonicotinic acid hydrazide derivatives with anti‐tubercular activity: Machine learning, molecular docking, synthesis and biological testing
10.1111/cbdd.13188 2018-03-14 The problem of designing new anti‐tubercular drugs against multiple‐drug‐resistant tuberculosis (MDR‐TB) was addressed using advanced machine learning methods. Since there are only few published measurements against MDR‐TB, we collected a large literature dat... |
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Synthesis and evaluation of pyridinium‐hydrazone derivatives as potential antitumoral agents
10.1111/cbdd.13177 2018-03-13 The hydrazones of 4‐hydrazinylpyridinium bearing alkylphenyl groups on pyridinium nitrogen were synthesized and evaluated for their cytotoxic activity against MCF‐7, PC3, U2OS, and HEK293 cell lines by Wst1 cell proliferation assay. Cytotoxic activity results... |