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Bioorganic & Medicinal Chemistry

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  1. Studies towards the synthesis of indolizin-5(3H)-one derivatives and related 6,5-azabicyclic scaffolds by ring-closing metathesis

    Bioorganic & Medicinal Chemistry (2013)

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  2. α-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one

    Bioorganic & Medicinal Chemistry (2012)

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  3. Effect of arginine methylation on the RNA recognition and cellular uptake of Tat-derived peptides

    Bioorganic & Medicinal Chemistry (2006)

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  4. Design, synthesis and decoration of molecular scaffolds for exploitation in the production of alkaloid-like libraries

    Bioorganic & Medicinal Chemistry (1992)

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  5. Synthesis, structural analysis and antitumor activity of novel 17α-picolyl and 17(E)-picolinylidene A-modified androstane derivatives.

    Bioorganic & Medicinal Chemistry 23(7):1557 (2015) PMID 25737400

    The heterocyclic ring at C-17 position of the androstane compounds plays an important role in biological activity. The aim of the present study was to synthesize and evaluate potential antitumor activity of different A-modified 17α-picolyl and 17(E)-picolinylidene androstane derivatives. In several...
  6. Synthesis and biological evaluation of 3-phenyl-3-aryl carboxamido propanoic acid derivatives as small molecule inhibitors of retinoic acid ...

    Bioorganic & Medicinal Chemistry 23(6):1356 (2015) PMID 25684424

    All-trans-retinoic acid (ATRA), the biologically active metabolite of vitamin A, is used medicinally for the treatment of hyperproliferative diseases and cancers. However, it is easily metabolized. In this study, the leading compound S8 was found based on virtual screening. To improve the activity o...
  7. Discovery of biphenyl-based VEGFR-2 inhibitors. Part 3: Design, synthesis and 3D-QSAR studies.

    Bioorganic & Medicinal Chemistry 23(5):1044 (2015) PMID 25637123

    We designed and synthesized 33 biphenyl amides based on our previously reported lead compound. The biological results indicated that four compounds (18b, 20e, 20h and 20j) are potent VEGFR-2 inhibitors which are comparable to positive control. Compound 18b displayed the most potent VEGFR-2 inhibitio...
  8. Synthesis of new ligands for targeting the S1P1 receptor.

    Bioorganic & Medicinal Chemistry 23(5):1011 (2015) PMID 25656338

    We developed new agonists for the S1P1 receptor. The biological activity was tested in vivo and promising ligands were fluorinated at different positions to identify candidates for positron emission tomography (PET) imaging after [(18)F]-labelling. The radioligands shall enable the imaging of S1P1 r...
  9. Furan-based acetylating agent for the chemical modification of proteins.

    Bioorganic & Medicinal Chemistry 23(4):791 (2015) PMID 25596165

    We have synthesized a furan-based acetylating agent, 2,5-bisacetoxymethylfuran (BAMF) from carbohydrate derived 5-hydroxymethylfurfural (HMF) and studied its acetylation activity with amines and cytochrome c. The results show that BAMF can modify proteins in biological conditions without affecting t...
  10. Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold.

    Bioorganic & Medicinal Chemistry 23(4):891 (2015) PMID 25596757

    A series of novel reversible BTK inhibitors was designed based on the structure of the recently reported preclinical drug RN486. Knowledge of the binding mode of RN486 led to the design of new inhibitors that utilized pyrrolo[2,3-d]pyrimidine to conformationally restrain key pharmacophoric groups wi...