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Bioorganic & Medicinal Chemistry

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  1. Chemical biology on the genome

    Bioorganic & Medicinal Chemistry 22(16):4356 (2014)

    Graphical abstract [Display omitted]
  2. 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...
  3. 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...
  4. Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors

    Bioorganic & Medicinal Chemistry 22(17):4882 (2014)

  5. A semi-synthetic derivative of artemisinin, artesunate inhibits prostaglandin E2 production in LPS/IFN╬│-activated BV2 microglia

    Bioorganic & Medicinal Chemistry 22(17):4726 (2014)

  6. Design, synthesis and biological evaluation of (E)-3-(3,4-dihydroxyphenyl)acrylylpiperazine derivatives as a new class of tubulin polymeriza...

    Bioorganic & Medicinal Chemistry 22(15):4285 (2014) PMID 24916028

    A series of novel (E)-3-(3,4-dihydroxyphenyl)acrylylpiperazine derivatives had been synthesized and evaluated their biological activities as potential tubulin polymerization inhibitors. Among these compounds, compound 3q exhibited potent antiproliferative activities against three cancer cell lines i...
  7. Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists. Pa...

    Bioorganic & Medicinal Chemistry 22(15):4323 (2014) PMID 24916029

    We previously reported that the novel dual 5-HT2B and 5-HT7 receptor antagonist N-(9-hydroxy-9H-fluorene-2-carbonyl)guanidine (4) exerted a suppressing effect on 5-HT-induced dural protein extravasation in guinea pigs. To develop a synthetic strategy, we performed docking studies of lead compound 4...
  8. Topoisomerase II inhibitors from the roots of Stellera chamaejasme L.

    Bioorganic & Medicinal Chemistry 22(15):4198 (2014) PMID 24931277

    Three new compounds, including one daphnane diterpene (1), one sesquiterpene (6), and one lignan (7) have been isolated from the Stellera chamaejasme L., together with five other known compounds, including four daphnane diterpenenoids (2-5) and one lignan (8). The structures of the new compounds wer...
  9. Straightforward entry to pyrido[2,3-d]pyrimidine-2,4(1H,3H)-diones and their ADME properties.

    Bioorganic & Medicinal Chemistry 22(15):3947 (2014) PMID 24984938

    A straightforward synthesis of pyrido[2,3-d]pyrimidine-2,4(1H,3H)-diones was developed starting from 2-chloropyridine-3-carboxylic acid by esterification, nucleophilic aromatic substitution and amide formation in one step, and ring closure allowing their synthesis with two identical or two different...
  10. Synthesis and evaluation of (E)-2-(acrylamido)cyclohex-1-enecarboxylic acid derivatives as HCA1, HCA2, and HCA3 receptor agonists.

    Bioorganic & Medicinal Chemistry 22(14):3654 (2014) PMID 24864041

    2-(3-(Naphthalen-2-yl)propanamido)cyclohex-1-enecarboxylic acid and its 6-hydroxynaphthalen-2-yl analogue are well-known hydroxyl-carboxylic acid (HCA) receptor HCA2 agonists. A series of novel aryl derivatives of 2-amidocyclohex-1-ene carboxylic acid that contained rigidity elements, such as an E-d...