Nuestros investigadores

Carlos Aydillo Miguel

Publicaciones científicas más recientes (desde 2010)

Autores: de Lucio, H. ; Moreno, Esther; et al.
Revista: ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
ISSN 0066-4804  Vol. 63  Nº 5  2019  págs. e02200-18
A novel series of thirty-one N-substituted urea, thiourea, and selenourea derivatives containing diphenyldiselenide entities were synthesized, fully characterized by spectroscopic and analytical methods, and screened for their in vitro leishmanicidal activities. The cytotoxic activity of these derivatives was tested against Leishmania infantum axenic amastigotes, and selectivity was assessed in human THP-1 cells. Thirteen of the synthesized compounds showed a significant antileishmanial activity, with 50% effective concentration (EC50) values lower than that for the reference drug miltefosine (EC50, 2.84 mu M). In addition, the derivatives 9, 11, 42, and 47, with EC50 between 1.1 and 1.95 mu M, also displayed excellent selectivity (selectivity index ranged from 12.4 to 22.7) and were tested against infected macrophages. Compound 11, a derivative with a cyclohexyl chain, exhibited the highest activity against intracellular amastigotes, with EC50 values similar to those observed for the standard drug edelfosine. Structure-activity relationship analyses revealed that N-aliphatic substitution in urea and selenourea is recommended for the leish-manicidal activity of these analogs. Preliminary studies of the mechanism of action for the hit compounds was carried out by measuring their ability to inhibit trypanothione reductase. Even though the obtained results suggest that this enzyme is not the target for most of these derivatives, their activity comparable to that of the standards
Autores: Aydillo, C; N. Mazo; C. D. Navo; et al.
Revista: CHEMBIOCHEM
ISSN 1439-4227  Vol. 20  Nº 10  2019  págs. 1246 - 1250
Autores: Ruberte, Ana Carolina; Plano, Daniel; Encio, I.; et al.
Revista: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN 0223-5234  Vol. 157  2018  págs. 14 - 27
Twenty-seven novel benzo[c][1,2,5]selenadiazole-5-carboxylic acid (BSCA) derivatives were designed and synthesized. Anti-proliferative activity of these structures was tested in vitro against a panel of five human cancer cell lines, including prostate (PC-3), colon (HT-29), leukemia (CCRF-CEM), lung (HTB-54) and breast (MCF-7). Four compounds (5, 6, 7 and 19) showed potent inhibitory activity with GI(50) values below 10 mu M in at least one of the cancer cell lines. The selectivity of these compounds was further examined in two non-malignant cell lines derived from breast (18465) and lung (BEAS-2B). Compound 7 exhibited promising anti-proliferative activity (GI(50) = 3.7 mu M) in MCF-7 cells, together with high selectivity index (SI> 27.1). The induction of cell death by compound 7 was independent of the apoptotic process and it did not affect cell cycle progression either. Likewise, radical scavenging properties of the new selenadiazole derivatives were confirmed by testing their ability to scavenge DPPH radicals. Four compounds (1, 2, 8 and 9) showed potent radical scavenging activity, compound 9 being the most effective. Overall, while compound 7 was identified as the most cell growth inhibitory agent and selectively toxic to cancer cells, compound 9 proved to be the most potent antioxidant among the selenadiazole derivatives synthesized. This series of compounds can serve as an excellent scaffold to achieve new and potent antioxidant compounds useful for several diseases, i.e. cancer, neurodegenerative, heart diseases and leishmaniasis, considering the high radical scavenging activity and low toxicity showed by most of the compounds. (C) 2018 Elsevier Masson SAS. All rights reserved.
Autores: V. Rojas-Ocáriz; I. Compañón; Aydillo, C; et al.
Revista: JOURNAL OF ORGANIC CHEMISTRY
ISSN 0022-3263  Vol. 81  Nº 14  2016  págs. 5929-5941
Autores: M. I. Gutiérrez-Jiménez; Aydillo, C; C. D. Navo; et al.
Revista: ORGANIC LETTERS
ISSN 1523-7060  Vol. 18  Nº 12  2016  págs. 2796-2799
Autores: Aydillo, C; I. Compañón; A. Avenoza, (Autor de correspondencia); et al.
Revista: JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
ISSN 0002-7863  Vol. 136  Nº 2  2014  págs. 789-800
Autores: G. Jiménez-Osés, (Autor de correspondencia); Aydillo, C; J. H. Busto; et al.
Revista: JOURNAL OF ORGANIC CHEMISTRY
ISSN 0022-3263  Vol. 79  Nº 6  2014  págs. 2556-2563
Autores: Aydillo, C; C. D. Navo; J. H. Busto; et al.
Revista: JOURNAL OF ORGANIC CHEMISTRY
ISSN 0022-3263  Vol. 78  Nº 21  2013  págs. 10968-10977
Autores: Aydillo, C; Avenoza A., (Autor de correspondencia); Busto, JH; et al.
Revista: ORGANIC LETTERS
ISSN 1523-7060  Vol. 14  Nº 1  2012  págs. 334-337
Autores: Aydillo, C; G. Jiménez-Osés; A. Avenoza, (Autor de correspondencia); et al.
Revista: JOURNAL OF ORGANIC CHEMISTRY
ISSN 0022-3263  Vol. 76  Nº 17  2011  págs. 6990-6996
Autores: S Ramos-Inza; Aydillo, C; C Sanmartín; et al.
Libro:  Heterocycles - Synthesis and Biological Activities
2019  págs. 1 - 21