SCIENTIFIC PAPERS

Wang, S.R.; Yang, C.G.; Sanchez-Murcia, P.A.; Snyder, J.P.; Yan, N.; Saez-Calvo, G.; Diaz, J.F.; Gago, F. and Fang, W.S. Restoration of Microtubule Interaction and Cytotoxicity in D-seco Taxanes upon Incorporation of 20-Hydroxymethyl-4-allyloxy Groups (2015) Org. Lett. 17, 24, 6098-6101

Canela, M.D., Bueno, O., Noppen, Sáez-Calvo, G., Estévez-Gallego, J., Díaz, J.F., Camarasa, M.J., Liekens, S.; Pérez-Pérez, M.J. and Priego E.M. Targeting the colchicine site in tubulin through cyclohexanedione derivatives. (2016) RSC Advances. 6, 19492

Canela, M.D., Noppen, S., Bueno, O., Prota, A.E., Bargsten, K., Sáez-Calvo, G. Jimeno, M.L., Ribatti, D.; Velázquez, S., Camarasa, M.J.; Díaz, J.F., Steinmetz, M.O.; Priego, E.M.; Pérez-Pérez M.J. and Liekens, S. Antivascular and antitumor properties of the tubulin-binding chalcone TUB091. (2016) Oncogene, in press.

Pera, B., Calvo-Vidal, M.N. Ambati, S., Jordi, M., Kahn, A., Díaz, J.F., Fang, W-S., Altmann, K-H. Cerchietti, L., Moore, M.A.S. High affinity and covalent-binding microtubule stabilizing agents show activity in chemotherapy-resistant acute myeloid leukemia cells.2015 Cancer Letters 368, 97–104.

Torijano-Gutiérrez, S., Concepción Vilanova, C. Santiago Díaz-Oltra, S Juan Murga, J. Eva Falomir, E., Carda, M., Redondo-Horcajo, M. Díaz, J.F., Barasoain, I, and Marco, J.A. The Mechanism of the Interactions of Pironetin Analog/Combretastatin A-4 Hybrids with Tubulin 2015 Arch. Pharm. Chem. Life Sci., 348, 541–547.

Alejandre-García, I., Álvarez, L., Cardoso-Taketa, A., González-Maya, L, Antúnez, M. Salas-Vidal, E., Díaz, J.F., Marquina-Bahena, S. and Villarreal, M.L. Cytotoxic Activity and Chemical Composition of the Root Extract from the Mexican Species Linum scabrellum: Mechanism of Action of the Active Compound 6-Methoxypodophyllotoxin 2015 Evidence-Based Complementary and Alternative Medicine Volume 2015, Article ID 298463, 11 pages

Alonso-Cristobal, P., Oton-Fernandez, O., Mendez-Gonzalez, D., Díaz, J.F., Lopez-Cabarcos, E. Barasoain, I. and Rubio-Retama, J. [2015] Synthesis, Characterization, and Application in HeLa Cells of an NIR Light Responsive Doxorubicin Delivery System Based on NaYF4:Yb,Tm@SiO2‑PEG Nanoparticles. ACS Appl. Mater. Interfaces In Press

Sánchez, D., Andreou,T., Costa, A.M., Meyer, K.G., Williams, D.R., Barasoain, I., Díaz,J.F., Lucena-Agell, D. and Vilarrasa,J. Total Synthesis of Amphidinolide K, a Macrolide that Stabilizes F‑Actin [2015] JOC in press.

Alejandre-García, I., Álvarez, L., Cardoso-Taketa, A., González-Maya, L., Antúnez, M., Salas-Vidal, E., Díaz, J. F., Marquina-Bahena, S. and Villarreal, M.L. [2015] Cytotoxic Activity and Chemical Composition of the Root Extract from the Mexican Species Linum scabrellum: Mechanism of Action of the Active Compound 6-Methoxypodophyllotoxin.
Evidence-Based Complementary and Alternative Medicine Volume 2015, Article

Pinar, M., Arst, H.N. Jr., Pantazopoulou, A., Tagua V.G., de los Ríos, V. Rodríguez-Salarichs, J., Díaz, J.F. and Peñalva, M.A. [2015] TRAPPII regulates exocytic Golgi exit by mediating nucleotide exchange on the Ypt31ortholog RabERAB11 PNAS 4346–4351, 112-114

Ibrahim Chaaban, I., El Khawass, E.M., Abd El Razik, H.A., El Salamouni, N.Redondo-Horcajo, M., Barasoain, I.Díaz, J.F. Yli-Kauhaluoma, J., Moreira, V.M., Synthesis and biological evaluation of new oxadiazoline-substituted naphthalenyl acetates as anticancer agents. European Journal of Medicinal Chemistry 87 (2014) 805e813 .

Prota A.E., Bargsten, K., Díaz, J.F., Marsh, M., Cuevas C., Liniger, M., Neuhaus, C., Andreu, J.M. Altmann, K.-H. and Steinmetz M.O. A new tubulin-binding site and pharmacophore for microtubule-destabilizing anticancer drugs. (2014) PNAS 111, 38, 13817-13821.

Canela, M.D., Perez-Perez, M.J., Sam Noppen, S., Sáez-Calvo, G., Díaz, J.F., Camarasa, M.J., Liekens, S. and Priego, E.M. Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach (2014) J. Med. Chem., 57, 3924-3938.

Gaugaz, F.Z., Redondo-Horcajo, M., Barasoain, I. Díaz, J.F. Cobos-Correa, A. Kaufmann, M. Altmann, K.H. The Impact of Cyclopropane Configuration on the Biological Activity of Cyclopropyl-Epothilones. (2014) ChemMedChem 9, 2227-2232.

Matesanz, R., Trigili, C., Rodríguez-Salarichs, J., Zanardi, I., Pera, B., Nogales, A., Fang, W-S. , Jímenez-Barbero, J., Canales, A. Barasoain, I.,Ojima, I., Díaz, J.F. Taxanes with high potency inducing tubulin assembly overcome tumoural cell resistances. (2014) Bioorganic and Medicinal Chemistry 22, 5078-5090.

Martínez-Díez M., Guillén-Navarro, M.J., Pera, B., Bouchet, B.P ,Martínez Leal J.F,Barasoain I., Cuevas C., Andreu, J.M., García Fernández, L.F., Díaz, J.F.Avilés, P., Galmarini, C.M. PM060184, a new tubulin binding agent with potent antitumor activity including P-glycoprotein over-expressing tumors (2014) Biochemical Pharmacology 88 291–302

Bras, W., Torbet, J., Diakun, G.P., Rikken, G.L.J.A. and Diaz, J. F. The diamagnetic susceptibility of the tubulin dimer (2014) Journal of Biophysics Volume 2014, Article ID 985082, 5 pages

Canales, A., Nieto, L., Rodríguez-Salarichs, J., Sánchez-Murcia, P.A., Claire Coderch, C., Cortés-Cabrera, A., Paterson, I., Carlomagno, T., Gago, F., Andreu, J.M., Altmann, K.H. Jiménez-Barbero, J. and Díaz, J.F. Molecular Recognition of Epothilones by Microtubules and Tubulin Dimers Revealed by Biochemical and NMR Approaches (2014) ACS Chem. Biol. 9 (4) 1033–1043

Prota, A.E., Bargsten, K., Northcote, P.T., Marsh, M, Altmann, K.H., Miller, J.H., Díaz, J.F. and Steinmetz, M.O. Structural Basis of Microtubule Stabilization by Laulimalide and Peloruside A (2014) Angew. Chem. Int. Ed., 53, 1621-1625,

Paños, J., Díaz-Oltra, S., Sánchez-Peris, M., García-Pla, J., Murga, J., Falomir, E., Carda, M., Redondo-Horcajo, M. Díaz, J.F., Barasoain, I. and J Marco, A., Synthesis and biological evaluation of truncated α-tubulin-binding pironetin analogues lacking alkyl pendants in the side chain or the dihydropyrone ring, (2013) Org. Biomol. Chem., 2013, 11, 5809- 5826

Pera, B., Barasoain, I., Canales, A., Matesanz, R., Rodriguez-Salarichs, J., García-Fernandez, L.F. Moneo, V. Jiménez-Barbero, J., Galmarini, C.M., Cuevas, C., Díaz, J.F and Andreu, J.M. New interfacial microtubule inhibitors of marine origin with potent antitumor activity and a distinct mechanism (2013) ACS Chemical Biology. 8, 284-294.

Álvarez, R., Puebla, P., Díaz, J.F., Bento, A.C., García-Navas, R., de la Iglesia-Vicente, J. Mollinedo, F., Andreu,J.M., Medarde, M. and Peláez, R. Endowing Indole-Based Tubulin Inhibitors with an Anchor for Derivatization: Highly Potent 3 Substituted Indolephenstatins and Indoleisocombretastatins, (2013) J. Med. Chem. 56, 2813−2827.

Coderch,C., Tang,Y., Klett, J. Zhang, S.E. Ma, Y.T., Wang, S., Matesanz, R., Pera, B., Canales, A. Jiménez-Barbero, J. Morreale, A, Díaz, J.F., Fang, W.S and Gago, F. A structure-based design of new C2- and C13-substituted taxanes: tubulin binding affinities and extended quantitative structure–activity relationships using comparative binding energy (COMBINE) analysis. (2013) Org. Biomol. Chem. 11, 3046

Field, J.J., Díaz, J.F. and Miller, J.H. The binding sites of microtubule-stabilizing agents. (2013) Chemistry and Biology. 20, 301-315.

Carda, M., Murga, J., Paños, J., Angulo-Pachón, C.A., García-Pla, J., Díaz-Oltra, S., Marco, J.A., Trigili, C., Redondo-Horcajo, C., Díaz, J.F. and Barasoain, I. Synthesis and Biological Evaluation As Microtubule-Active Agents of Several Tetrahydrofuran and Spiroacetal Derivatives. (2013) Current Medicinal Chemistry. 20, 1173-1182.

Maccari, G., Mori, M. Rodríguez-Salarichs, J., Fang, W.S., Díaz, J.F. and Botta, M. Free Energy Profile and Kinetics. Studies of Paclitaxel Internalization from the Outer to the Inner Wall of Microtubules (2013) J. Chem. Theory Comput. 2013, 9, 698−706.

Carda, M., Murga, J., Díaz-Oltra, S., García-Pla, J., Paños, J., Falomir, E. Trigili, C., Díaz, J.F., Barasoain, I. and Marco, J.A. Synthesis and Biological Evaluation of α-Tubulin-Binding Pironetin Analogues with Enhanced Lipophilicity (2013) Eur. J. Org. Chem. 1116-1123.

Prota, A.E., Bargsten, K., Zurwerra, D., Field,J.J., Díaz, J.F. Altmann, K.H. and Steinmetz, M.O. Molecular Mechanism of Action of Microtubule-Stabilizing Anticancer Agents, Science (2013) 339, (6119) 587-590.

Fournier-Dit-Chabert, J., Vinader, V., Santos, A.R., Redondo-Horcajo, M., Dreneau, A., Ramkrishna Basak, R., Cosentino, L., Marston, G., Abdel-Rahman, H., Loadman, P.M., Shnyder, S.D., Díaz, J.F., Barasoain, I., Falconer, R. A. and Pors K. (2012) Synthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation Bioorganic & Medicinal Chemistry Letters 22 (2012) 7693–7696,

Cosentino, L., Redondo-Horcajo, M., Zhao, Y., Santos, A.R., Chowdury, K.F., Vinader, V., Abdallah, Q.M.A., Abdel-Rahman, H., Fournier-Dit-Chabert, J., Shnyder, S., Loadman, P.M., Fang,W. S., Díaz, J.F., Barasoain, I., Burns P.A. and Pors, K. (2012) Synthesis and Biological Evaluation of Colchicine B‑Ring Analogues Tethered with Halogenated Benzyl Moieties. J. Med. Chem. 55 (24), pp 11062–11066.

10.1016/j.ejmech.2012.06.045.

Field, J.J., Pera, B.*, Calvo, E*, Canales, A., Zurwerra, D., Trigili, C, Rodríguez-Salarichs, J., Matesanz, R., Kanakkanthara, A., Wakefield, S., Singh, A.J., Jiménez-Barbero, J., Northcote, P., Miller, J.H., López, J.A., Hamel, E., Barasoain, I., Altmann, K.H. and Díaz, J.F. (2012) Zampanolide, a potent new microtubule stabilizing agent, covalently reacts with the taxane luminal site in both tubulin αβ-heterodimers and microtubules. Chemistry and Biology. 19, 686–698.

Coderch, C., Klett, J., Morreale, A., Díaz, J.F. and Gago, F. Comparative Binding Energy (COMBINE) Analysis Supports a Proposal for the Binding Mode of Epothilones to β-Tubulin. ChemMedChem (2012) 7, 836-843

Bennani, Y.L. Gu, W., Canales, A., Díaz, J.F., Eustace, B. K. Hoover, R.R., Jiménez-Barbero, J., Nezami, A. and Wang, T. Tubulin Binding, Protein-Bound Conformation in Solution, and Antimitotic Cellular Profiling of Noscapine and Its Derivatives. J. Med. Chem. (2012), 55, 1920-1925.

Calvo, E., Barasoain, I., Matesanz, R., Pera, B., Camafeita, E., Pineda, O., Hamel, E., Vanderwal, C. D.José Manuel Andreu, Juan A. López and José Fernando Díaz Cyclostreptin Derivatives Specifically Target Cellular Tubulin and Further Map the Paclitaxel Site, Biochemistry (2012) 51, 329-341.

Matesanz, R., Diaz, J.F., Corzana, F., Santana, A.G., Bastida, A, Asensio J.L. Multiple keys for a single lock: the unusual structural plasticity of the Nucleotidyltransferase (4’)/kanamycin complex Chemistry. A European Journal (2012) 18, 2875-2889.