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Journal of Medicinal Chemistry

  1. Trisubstituted Pyrimidines as Efficacious and Fast-acting Antimalarials

    Fairlamb, A. H. , Gilbert, I. H. & 28 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., 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

  2. 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

  3. 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

  4. 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

  5. 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

  6. 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

  7. 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

  8. 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

  9. 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

  10. 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. 59, 4, p. 1492-1500 9 p.

    Research output: Contribution to journalArticle

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