Journal of medicinal chemistry

(ISSN: 0022-2623, 1520-4804)

Table of Contents

2014 - 57 (13)

  • Beyond affinity: enthalpy-entropy factorization unravels complexity of a flat structure-activity relationship for inhibition of a tRNA-modifying enzyme. 
  • Chasing protons: how isothermal titration calorimetry, mutagenesis, and pKa calculations trace the locus of charge in ligand binding to a tRNA-binding enzyme. 
  • Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides. 
  • Easily accessible polycyclic amines that inhibit the wild-type and amantadine-resistant mutants of the M2 channel of influenza A virus. 
  • New orally active dual enkephalinase inhibitors (DENKIs) for central and peripheral pain treatment. 
  • Discovery and structure-activity relationship of novel 2,3-dihydrobenzofuran-7-carboxamide and 2,3-dihydrobenzofuran-3(2H)-one-7-carboxamide derivatives as poly(ADP-ribose)polymerase-1 inhibitors. 
  • A low cytotoxic cationic metal-organic framework carrier for controllable drug release. 
  • SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase. 
  • Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors. 
  • Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. 
  • Aminoazabenzimidazoles, a novel class of orally active antimalarial agents. 
  • Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu���). 
  • Maximizing diversity from a kinase screen: identification of novel and selective pan-Trk inhibitors for chronic pain. 
  • Multistage screening reveals chameleon ligands of the human farnesyl pyrophosphate synthase: implications to drug discovery for neurodegenerative diseases. 
  • Organometallic nucleoside analogues with ferrocenyl linker groups: synthesis and cancer cell line studies. 
  • Efficient modulation of ��-aminobutyric acid type A receptors by piperine derivatives. 
  • Ethyl 1,8-naphthyridone-3-carboxylates downregulate human papillomavirus-16 E6 and E7 oncogene expression. 
  • Design, synthesis, and biological evaluations of tumor-targeting dual-warhead conjugates for a taxoid-camptothecin combination chemotherapy. 
  • In vivo long-term magnetic resonance imaging activity of ferritin-based magnetic nanoparticles versus a standard contrast agent. 
  • Synthesis and biological activities of novel pleuromutilin derivatives with a substituted thiadiazole moiety as potent drug-resistant bacteria inhibitors. 
  • Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT��� and dopamine D��� receptor ligands. 
  • Lead optimization of 1,4-azaindoles as antimycobacterial agents. 
  • Undecaprenyl diphosphate synthase inhibitors: antibacterial drug leads. 
  • Importance of sphingosine kinase (SphK) as a target in developing cancer therapeutics and recent developments in the synthesis of novel SphK inhibitors. 
  • Foundation-directed therapeutic development in Huntington's disease. 
  • Switching invariant natural killer T (iNKT) cell response from anticancerous to anti-inflammatory effect: molecular bases. 
  • Discovery of innovative therapeutics: today's realities and tomorrow's vision. 2. Pharma's challenges and their commitment to innovation. 
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