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Bioorganic & Medicinal Chemistry

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  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. Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping

    Bioorganic & Medicinal Chemistry 22(21):6256 (2014)

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  4. Synthesis of IB-01212 by multiple N-methylations of peptide bonds

    Bioorganic & Medicinal Chemistry 22(21):6156 (2014)

  5. Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonis...

    Bioorganic & Medicinal Chemistry 22(21):6026 (2014)

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  6. Human α1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines

    Bioorganic & Medicinal Chemistry 22(21):5910 (2014)

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  7. 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...
  8. 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...
  9. 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...
  10. 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...