Discovery - University of Dundee - Online Publications

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Journal of Medicinal Chemistry

  1. Characterization of 2,4-Diamino-6-oxo-1,6-dihydropyrimidin-5-yl Ureido based inhibitors of Trypanosoma brucei FolD and testing for antiparasitic activity

    Eadsforth, T. C., Pinto, A., Luciani, R., Tamborini, L., Cullia, G., De Micheli, C., Marinelli, L., Cosconati, S., Novellino, E., Lo Presti, L., Cordeiro Da Silva, A., Conti, P., Hunter, W. N. & Costi, M. P. 22 Oct 2015 In : Journal of Medicinal Chemistry. 58, 20, p. 7938-7948 11 p.

    Research output: Contribution to journalArticle

  2. Discovery of indoline-2-carboxamide derivatives as a new class of brain-penetrant inhibitors of Trypanosoma brucei

    Cleghorn, L. A. T., Albrecht, S., Stojanovski, L., Simeons, F. R. J., Norval, S., Kime, R., Collie, I. T., De Rycker, M., Campbell, L., Hallyburton, I., Frearson, J. A., Wyatt, P. G., Read, K. D. & Gilbert, I. H. 8 Oct 2015 In : Journal of Medicinal Chemistry. 58, 19, p. 7695-7706 12 p.

    Research output: Contribution to journalArticle

  3. Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): a potent, orally available, and highly selective PARP-1 inhibitor for cancer therapy

    Papeo, G. , Posteri, H. , Borghi, D. , Busel, A. A. , Caprera, F. , Casale, E. , Ciomei, M. , Cirla, A. , Corti, E. , D'Anello, M. , Fasolini, M. , Forte, B. , Galvani, A. , Isacchi, A. , Khvat, A. , Krasavin, M. Y. , Lupi, R. , Orsini, P. , Perego, R. , Pesenti, E. & 9 others Pezzetta, D., Rainoldi, S., Riccardi-Sirtori, F., Scolaro, A., Sola, F., Zuccotto, F., Felder, E. R., Donati, D. & Montagnoli, A. 10 Sep 2015 In : Journal of Medicinal Chemistry. 58, 17, p. 6875-6898 24 p.

    Research output: Contribution to journalArticle

  4. Development of selective covalent Janus kinase 3 inhibitors

    Tan, L., Akahane, K., McNally, R., Reyskens, K. M. S. E., Ficarro, S. B., Liu, S., Herter-Sprie, G. S., Koyama, S., Pattison, M. J., Labella, K., Johannessen, L., Akbay, E. A., Wong, K. K., Frank, D. A., Marto, J. A., Look, T. A., Arthur, J. S. C., Eck, M. J. & Gray, N. S. 27 Aug 2015 In : Journal of Medicinal Chemistry. 58, 16, p. 6589-6606 18 p.

    Research output: Contribution to journalArticle

  5. New monocyclic, bicyclic, and tricyclic ethynylcyanodienones as activators of the Keap1/Nrf2/ARE pathway and inhibitors of inducible nitric oxide synthase

    Li, W., Zheng, S., Higgins, M., Morra, R. P., Mendis, A. T., Chien, C-W., Ojima, I., Mierke, D. F., Dinkova-Kostova, A. T. & Honda, T. 11 Jun 2015 In : Journal of Medicinal Chemistry. 58, 11, p. 4738-4748 11 p.

    Research output: Contribution to journalArticle

  6. Structural characterization of LRRK2 inhibitors

    Gilsbach, B. K., Messias, A. C., Ito, G., Sattler, M., Alessi, D. R., Wittinghofer, A. & Kortholt, A. 14 May 2015 In : Journal of Medicinal Chemistry. 58, 9, p. 3751-3756 6 p.

    Research output: Contribution to journalArticle

  7. New synthetic routes to Triazolo-benzodiazepine analogues: expanding the scope of the bump-and-hole approach for selective Bromo and Extra-Terminal (BET) bromodomain inhibition

    Baud, M. G. J., Lin-Shiao, E., Zengerle, M., Tallant, C. & Ciulli, A. 2015 In : Journal of Medicinal Chemistry. 9 p.

    Research output: Contribution to journalArticle

  8. Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von hippel-lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities

    Galdeano , C., Gadd, M. S., Soares, P., Scaffidi, S., Van Molle, I., Birced, I., Hewitt, S., Dias, D. M. & Ciulli, A. 23 Oct 2014 In : Journal of Medicinal Chemistry. 57, 20, p. 8657-8663 7 p.

    Research output: Contribution to journalArticle

  9. The design and synthesis of potent and selective inhibitors of trypanosoma brucei glycogen synthase kinase 3 for the treatment of human African trypanosomiasis

    Urich, R., Grimaldi, R., Luksch, T., Frearson, J. A., Brenk, R. & Wyatt, P. G. 25 Sep 2014 In : Journal of Medicinal Chemistry. 57, 18, p. 7536-7549 14 p.

    Research output: Contribution to journalArticle

  10. Structure-based design and synthesis of antiparasitic pyrrolopyrimidines targeting pteridine reductase 1

    Khalaf, A. I., Huggan, J. K., Suckling, C. J., Gibson, C. L., Stewart, K., Giordani, F., Barrett, M. P., Wong, P. E., Barrack, K. L. & Hunter, W. N. 14 Aug 2014 In : Journal of Medicinal Chemistry. 57, 15, p. 6479-6494 16 p.

    Research output: Contribution to journalArticle

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