Discovery - University of Dundee - Online Publications

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Journal of Medicinal Chemistry

  1. Discovery of a quinoline-4-carboxamide derivative with a novel mechanism of action, multistage antimalarial activity, and potent in vivo efficacy

    Gilbert, I. H. & 26 others Baragaña, B., Norcross, N. R., Wilson, C., Porzelle, A., Hallyburton, I., Grimaldi, R., Osuna-Cabello, M., Norval, S., Riley, J., Stojanovski, L., Simeons, F. R. C., Wyatt, P. G., Delves, M. J., Meister, S., Duffy, S., Avery, V. M., Winzeler, E. A., Sinden, R. E., Wittlin, S., Frearson, J. A., Gray, D. W., Fairlamb, A. H., Waterson, D., Campbell, S. F., Willis, P. & Read, K. D. 10 Nov 2016 In : Journal of Medicinal Chemistry. 59, 21, p. 9672-9685 14 p.

    Research output: Contribution to journalArticle

  2. Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides

    Thomas, J. & 25 others Russell, S., Rahmani, R., Jones, A. J., Newson, H. L., Neilde, K., Cotillo, I., Rahmani Khajouei, M., Ferrins, L., Qureishi, S., Nguyen, N., Martinez-Martinez, M. S., Weaver, D. F., Kaiser, M., Riley, J., De Rycker, M., Read, K. D., Flematti, G. R., Ryan, E., Tanghe, S., Rodriguez, A., Charman, S. A., Kessler, A., Avery, V. M., Baell, J. B. & Piggott, M. J. 10 Nov 2016 In : Journal of Medicinal Chemistry. 59, 21, p. 9686-9720 35 p.

    Research output: Contribution to journalArticle

  3. From Companion Diagnostics to Theranostics: A New Avenue for Alzheimer's Disease?

    Bolognesi, M. L., Gandini, A., Prati, F. & Uliassi, E. 8 Sep 2016 In : Journal of Medicinal Chemistry. 59, 17, p. 7759-7770 12 p.

    Research output: Contribution to journalReview article

  4. Trisubstituted Pyrimidines as Efficacious and Fast-acting Antimalarials

    Gilbert, I. H. & 29 others Norcross, N. R., Baragana, B., Wilson, C., Hallyburton, I., Osuna-Cabello, M., Norval, S., Riley, J., Stojanovski, L., Simeons, F. R. C., Porzelle, A., Grimaldi, R., Wittlin, S., Duffy, S., Avery, V. M., Meister, S., Sanz, L., Jimenez-Diaz, B., Angulo-Barturen, I., Ferrer, S., Santos Marinez, M., Javier Gamo, F., Frearson, J. A., Gray, D. W., Fairlamb, A. H., Winzeler, E. A., Waterson, D., Campbell, S. F., Willis, P. & Read, K. D. 14 Jul 2016 In : Journal of Medicinal Chemistry. 59, 13, p. 6101-6120 20 p.

    Research output: Contribution to journalArticle

  5. 4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1)

    Hügle, M., Lucas, X., Weitzel, G., Ostrovskyi, D., Breit, B., Gerhardt, S., Einsle, O., Günther, S. & Wohlwend, D. 25 Feb 2016 In : Journal of Medicinal Chemistry. 59, 4, p. 1518-1530 13 p.

    Research output: Contribution to journalArticle

  6. 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. 25 Feb 2016 In : Journal of Medicinal Chemistry. 59, 4, p. 1492-1500 9 p.

    Research output: Contribution to journalArticle

  7. 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

  8. 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

  9. Design, synthesis, and evaluation of triazole derivatives that induce Nrf2 dependent gene products and inhibit the Keap1-Nrf2 protein-protein interaction

    Bertrand, H. C., Schaap, M., Baird, L., Georgakopoulos, N. D., Fowkes, A., Thiollier, C., Kachi, H., Dinkova-Kostova, A. T. & Wells, G. 24 Sep 2015 In : Journal of Medicinal Chemistry. 58, 18, p. 7186-7194 9 p.

    Research output: Contribution to journalArticle

  10. 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. & 10 others Pesenti, E., 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

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