Advanced search×

Bioorganic & Medicinal Chemistry

Print ISSN
Electronic ISSN
Impact factor
Usage rank
Article count
Free count
Free percentage
PDFs via platforms
Sciencedirect from 1993, Proquest, Rcgp, Ingenta, Gale, and CSA

  1. The effect of C(5) cytosine methylation at CpG sequences on mitomycin-DNA bonding profiles.

    Bioorganic & Medicinal Chemistry 9(4):863 (2001) PMID 11354669

    We have determined the bonding profiles for mitomycin monoalkylation in two DNA restriction fragments where the CpG sequences were methylated. Three mitomycin substrates were used and two different enzymatic assays employed to monitor the extent of drug modification at the individual base sites. Dru...
  2. TRH mimetics: differentiation of antiamnesic potency from antidepressant effect.

    Bioorganic & Medicinal Chemistry 5(11):2029 (1997) PMID 9416420

    We were pursuing an approach that consists of two steps: (1) 'obligatory' replacement of histidine with glutamine in TRH and (2) the application of conformational constraints for putative bioactive conformation I stabilized by an intramolecular hydrogen bond between C-terminal carboxamide proton and...
  3. Design, synthesis and biological evaluation of novel 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives as ...

    Bioorganic & Medicinal Chemistry 22(19):5141 (2014) PMID 25189690

    Hydroxylated 6H-benzo[c]chromen-6-one derivatives (i.e., urolithins) are the main bioavailable metabolites, and biomarkers of ellagitannins present in various nutrition. Although these dietaries, the sources of urolithins, are employed in folk medicine as cognitive enhancer in the treatment of Alzhe...
  4. Design, synthesis and biological evaluation of 3,5-disubstituted 2-amino thiophene derivatives as a novel class of antitumor agents.

    Bioorganic & Medicinal Chemistry 22(18):5097 (2014) PMID 24398384 PMCID PMC4170804

    We designed a novel series of agents based on the 2-amino-3-alkoxycarbonyl/cyano-5-arylethylthiophene scaffold. The presence of the ethyl spacer between the 2',5'-dimethoxyphenyl and the 5-position of the thiophene ring, as well as the number and location of methoxy substitutents on the phenyl ring,...
  5. Synthesis of fluorinated agonist of sphingosine-1-phosphate receptor 1.

    Bioorganic & Medicinal Chemistry 22(17):4955 (2014) PMID 25047939

    The bioactive metabolite sphingosine-1-phosphate (S1P), a product of sphingosine kinases (SphKs), mediates diverse biological processes such as cell differentiation, proliferation, survival and angiogenesis. A fluorinated analogue of S1P receptor agonist has been synthesized by utilizing a ring open...
  6. Cytotoxicity of synthesized 1,4-naphthoquinone analogues on selected human cancer cell lines.

    Bioorganic & Medicinal Chemistry 22(17):5013 (2014) PMID 25059501

    In an effort to establish new candidates with enhanced anticancer activity of 5-hydroxy-7-methyl-1,4-naphthoquinone scaffold (7-methyljuglone) previously isolated from the root extract of Euclea natalensis, a series of 7-methyljuglone derivatives have been synthesized and assessed for cytotoxicity o...
  7. Discovery of quinazolin-4-amines bearing benzimidazole fragments as dual inhibitors of c-Met and VEGFR-2.

    Bioorganic & Medicinal Chemistry 22(17):4735 (2014) PMID 25082515

    Both c-Met and VEGFR-2 are important targets for the treatment of cancers. In this study, a series of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinazolin-4-amine derivatives were designed and identified as dual c-Met and VEGFR-2 inhibitors. Among these compounds bearing quinazoline and benzimidazole fra...
  8. Identification of novel inhibitors of phospho-MurNAc-pentapeptide translocase MraY from library screening: Isoquinoline alkaloid michellamin...

    Bioorganic & Medicinal Chemistry 22(17):4566 (2014) PMID 25127465

    The National Cancer Institute (NCI) Diversity Set was screened for potential inhibitors of phospho-MurNAc-pentapeptide translocase MraY from Escherichia coli using a primary fluorescence enhancement assay, followed by a secondary radiochemical assay. One new MraY inhibitor was identified from this s...
  9. Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.

    Bioorganic & Medicinal Chemistry 22(17):4924 (2014) PMID 25129171

    We present the discovery and optimization of ethyl 5-(piperazin-1-yl) benzofuran-2-carboxylate series of mycobacterial DNA gyraseB inhibitors, selected from Birla Institute of Technology and Science (BITS) database chemical library of about 3000 molecules. These compounds were tested for their biolo...
  10. Synthesis and biological activity of new salicylanilide N,N-disubstituted carbamates and thiocarbamates.

    Bioorganic & Medicinal Chemistry 22(15):4073 (2014) PMID 24953953

    We investigated the inhibitory effect of these compounds on mycobacterial isocitrate lyase and cellular toxicity. The minimum inhibitory concentrations (MICs) against mycobacteria were from 4 μM for thiocarbamates and from 16 μM for carbamates. Gram-positive bacteria, including methicillin-resistant...