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Journal of Medicinal Chemistry

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  1. Synthesis and structure-activity relationship studies of novel dual inhibitors of soluble epoxide hydrolase and 5-lipoxygenase.

    Journal of Medicinal Chemistry 56(4):1777 (2013) PMID 23356879

    We therefore designed and synthesized a library of hybrid molecules incorporating an imidazo[1,2-a]pyridine and an urea moiety as novel soluble epoxide hydrolase (sEH)/5-lipoxygenase (5-LO) dual inhibitors. Evaluation of the compounds was accomplished by in vitro testing using recombinant enzyme ass...
  2. Factors influencing the specificity of inhibitor binding to the human and malaria parasite dihydroorotate dehydrogenases.

    Journal of Medicinal Chemistry 55(12):5841 (2012) PMID 22621375

    The de novo pyrimidine biosynthesis enzyme dihydroorotate dehydrogenase is an emerging drug target for the treatment of malaria. In this context a key property of Plasmodium falciparum DHODH (PfDHODH) is that it can be selectively inhibited over its human homologue (HsDHODH). However...
  3. Design, synthesis, and pharmacological evaluation of glutamate carboxypeptidase II (GCPII) inhibitors based on thioalkylbenzoic acid scaffol...

    Journal of Medicinal Chemistry 55(12):5922 (2012) PMID 22642259

    A series of thiol-based glutamate carboxypeptidase II (GCPII) inhibitors have been synthesized with either a 3-(mercaptomethyl)benzoic acid or 2-(2-mercaptoethyl)benzoic acid scaffold. Potent inhibitors were identified from each of the two scaffolds with IC(50) values in the single-d...
  4. Nonhematotoxic naphthalene diimide modified by polyamine: synthesis and biological evaluation.

    Journal of Medicinal Chemistry 55(7):3502 (2012) PMID 22428910

    With the aim of up-regulating antitumor efficacy and down-regulating adverse effects, three types of aromatic imide and diimides were designed to couple with different polyamines. The in vitro assays revealed that two naphthalene diimide-polyamine conjugates could inhibit the growth of multiple cance...
  5. Identification of small molecule inhibitors of the HIV-1 nucleocapsid-stem-loop 3 RNA complex.

    Journal of Medicinal Chemistry 55(9):4132 (2012) PMID 22480197

    We have used SL3 RNA as a target for identification of small molecule inhibitors of the interactions of nucleocapsid protein (NCp7) and ψ-RNA. We report the use of computational and high-throughput screening approaches to identify sixteen compounds that bind SL3 RNA with micromolar affinities. Amon...
  6. Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants.

    Journal of Medicinal Chemistry 55(7):3021 (2012) PMID 22471376

    We further explored this motif by synthesizing additional urea-based inhibitors and by characterizing them in replicase HCV protease-resistant mutants assay. Several compounds, exemplified by 12, were found to be more potent in HCV replicon assays than leading second generation inhibitors such as da...
  7. First-in-class, dual-action, 3,5-disubstituted indole derivatives having human nitric oxide synthase (nNOS) and norepinephrine reuptake inhi...

    Journal of Medicinal Chemistry 55(7):3488 (2012) PMID 22420844

    A family of different 3,5-disubstituted indole derivatives having 6-membered rings were designed, synthesized and demonstrated inhibition of human nitric oxide synthase (NOS) with norepinephrine reuptake inhibitory activity (NERI). The structure activity relationship (SAR) within the...
  8. Design, synthesis, and in vitro activity of novel 2'-O-substituted 15-membered azalides.

    Journal of Medicinal Chemistry 55(7):3216 (2012) PMID 22380766

    We present a novel approach to the development of the azalide class of antimalarials by describing the design, synthesis and characterisation of novel 2'-O-substituted-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A derivatives consisting of different quinoline moieties covalently liked to a 15-membe...
  9. Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.

    Journal of Medicinal Chemistry 55(1):106 (2012) PMID 22148838

    Nonpeptidic, bivalent Smac mimetics designed based upon monovalent Smac mimetics with a diazabicyclic core structure bind to XIAP, cIAP1, and cIAP2 with low to subnanomolar affinities and are highly effective in antagonizing XIAP in cell-free functional assays. They efficiently induc...
  10. NHC gold halide complexes derived from 4,5-diarylimidazoles: synthesis, structural analysis, and pharmacological investigations as potential...

    Journal of Medicinal Chemistry 54(24):8605 (2011) PMID 22091836

    A series of novel neutral NHC gold halide complexes derived from 4,5-diarylimidazoles were synthesized, characterized and analyzed for biological effects. High growth inhibitory effects in MCF-7 and MDA-MB 231 breast cancer as well as HT-29 colon cancer cell lines depended on the pre...