Instituto Canario Of Investigacion Del Cancer

Las Palmas de Gran Canaria, Spain

Instituto Canario Of Investigacion Del Cancer

Las Palmas de Gran Canaria, Spain
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Lahoz F.,University of La Laguna | Oton C.J.,Polytechnic University of Valencia | Oton C.J.,Sant'Anna School of Advanced Studies | Lopez D.,University of La Laguna | And 6 more authors.
Optics Letters | Year: 2012

Optofluidic lasers have emerged as a new research field over the past few years. Most frequently they use conventional dye molecules as the gain medium. In this Letter, we demonstrate a laser emission produced by the coupling of the evanescent whispering gallery modes that resonate in a cylindrical microresonator to a newly developed gain medium. This medium is formed by attachment of a 7-nitrobenzo [c] [1,2,5]-oxadiazol-4-yl fluorescent tag to tamoxifen, the most widely used drug in the treatment of breast cancer. The antitumor character of the gain medium paves the way to novel biophotonic applications. © 2012 Optical Society of America.


Acero N.,University of San Pablo - CEU | Brana M.F.,Instituto Canario Of Investigacion Del Cancer | Anorbe L.,University of San Pablo - CEU | Dominguez G.,University of San Pablo - CEU | And 3 more authors.
European Journal of Medicinal Chemistry | Year: 2012

A novel series of indolocarbazoles were synthesized and their antiproliferative activity against HUVEC, LoVo, DLD-1 and ST-486 cell lines, was investigated. Those staurosporine analogs in which a substituted dimethylaminoalkoxy chain was attached to the indolic nitrogen showed interesting activity and selectivity with respect to HUVEC proliferation. The effect on capillary tube formation in 3-dimensional matrigel matrix was studied using the most active compounds. Evaluation of their in vivo anti-angiogenic activity in a murine Lewis lung cancer model was also analyzed. © 2011 Elsevier Ltd. All rights reserved.


Tejedor D.,CSIC - Institute of Natural Products and Agrobiology | Tejedor D.,Instituto Canario Of Investigacion Del Cancer | Lopez-Tosco S.,CSIC - Institute of Natural Products and Agrobiology | Lopez-Tosco S.,Instituto Canario Of Investigacion Del Cancer | And 3 more authors.
Chemistry - A European Journal | Year: 2010

Dominos! The multivalent reactivity profile of tertiary skipped diynes has been conveniently exploited in the domino and diversity-oriented synthesis of fully substituted pyrazoles and 1, 4-diazepane derivatives (see scheme). The developed manifold is chemically efficient and simple to operate. In addition, the resulting Ncontaining heterocycles are obtained in a regio- and chemoselective manner. (Chemical Equation Presented) © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.


Velazquez D.G.,University of La Laguna | Velazquez D.G.,Instituto Canario Of Investigacion Del Cancer | Luque R.,University of Cordoba, Spain
Tetrahedron Letters | Year: 2011

A rapid and efficient methodology to highly functionalised molecular units well suited as scaffolds for diversity-oriented molecular construction in the synthesis of natural products is reported herein. A key macrocyclic intermediate in the synthesis of the neo-clerodane diterpene (-)-teubrevin G was successfully synthesized in a 5-step sequence in a 70% overall yield using a novel intramolecular coupling between an allylborating agent and a 1,5-dialdehyde moiety. © 2011 Elsevier Ltd. All rights reserved.


Tejedor D.,CSIC - Institute of Natural Products and Agrobiology | Tejedor D.,Instituto Canario Of Investigacion Del Cancer | Mendez-Abt G.,CSIC - Institute of Natural Products and Agrobiology | Mendez-Abt G.,Instituto Canario Of Investigacion Del Cancer | And 2 more authors.
Chemistry - A European Journal | Year: 2010

A convenient domino access to substituted alkyl 1,2-dihydropyridine-3- carboxylates from propargyl enol ethers and primary amines was reported. A solution of propargyl sinyl ether 1a and p-anisidine in toluene was placed in a microwave-special closed vial and the solution was irradiated for 30 minutes in a single-mode microwave oven. The reaction mixture was dried over anhydrous sodium sulfate and filtrated using dichloromethane as solvent. After removing the solvent at reduced pressure the products were purified by flash column chromatography. Accordingly, the microwave irradiation of an ethanolic mixture of propargyl enol ether 1 a and MeONH2.HCl in the presence of NaOAc yielded the methyl 2-phenyl-4-pyridinecarboxylate in a convenient 54% yield. These results seem to point out to a new reaction pathway involving different thermally-driven rearrangements of the 2,4-dienal 3 intermediate.


Lara P.C.,Hospital Universitario Of Gran Canaria Dr Negrin | Lara P.C.,University of Las Palmas de Gran Canaria | Lara P.C.,Instituto Canario Of Investigacion Del Cancer | Pruschy M.,University of Zürich | And 4 more authors.
Radiation Oncology | Year: 2011

Vaults are evolutionary highly conserved ribonucleoproteins particles with a hollow barrel-like structure. The main component of vaults represents the 110 kDa major vault protein (MVP), whereas two minor vaults proteins comprise the 193 kDa vault poly(ADP-ribose) polymerase (vPARP) and the 240 kDa telomerase-associated protein-1 (TEP-1). Additionally, at least one small and untranslated RNA is found as a constitutive component. MVP seems to play an important role in the development of multidrug resistance. This particle has also been implicated in the regulation of several cellular processes including transport mechanisms, signal transmission and immune responses. Vaults are considered a prognostic marker for different cancer types. The level of MVP expression predicts the clinical outcome after chemotherapy in different tumour types. Recently, new roles have been assigned to MVP and vaults including the association with the insulin-like growth factor-1, hypoxia-inducible factor-1alpha, and the two major DNA double-strand break repair machineries: non-homologous endjoining and homologous recombination. Furthermore, MVP has been proposed as a useful prognostic factor associated with radiotherapy resistance. Here, we review these novel actions of vaults and discuss a putative role of MVP and vaults in the response to radiotherapy. © 2011 Lara et al; licensee BioMed Central Ltd.


Tejedor D.,CSIC - Institute of Natural Products and Agrobiology | Tejedor D.,Instituto Canario Of Investigacion Del Cancer | Cotos L.,CSIC - Institute of Natural Products and Agrobiology | Garcia-Tellado F.,CSIC - Institute of Natural Products and Agrobiology
Organic Letters | Year: 2011

Tertiary propargyl vinyl ethers armed with an electron-withdrawing group (amide or ester) at the tertiary propargylic position have been efficiently transformed into trisubstituted C 2-chain functionalized furans. The metal-free domino transformation involves a microwave-assisted tandem [3,3]-propargyl Claisen rearrangement/5-exo-dig O-cyclization reaction. The manifold can be performed in a one-pot fashion from the primary components (1,2-ketoester/1,2-ketoamide or tertiary propargyl alcohols). © 2011 American Chemical Society.


Rubio S.,Instituto Canario Of Investigacion Del Cancer | Leon F.,CSIC - Institute of Natural Products and Agrobiology | Quintana J.,Instituto Canario Of Investigacion Del Cancer | Cutler S.,University of Mississippi | Estevez F.,Instituto Canario Of Investigacion Del Cancer
European Journal of Medicinal Chemistry | Year: 2012

A new class of methyl esters of flavonoids, with different substituents on the B ring were synthesized and evaluated for their antiproliferative activity against the human leukemia cell line HL-60. The presence of either a methyl group (1f) or a chlorine atom (1o) at position 2′ of the B ring played an important role in affecting antiproliferative activity. The cytotoxic effects of these compounds were accompanied by the concentration- and time-dependent appearance of DNA- and nuclear-fragmentation, increase in the percentage of sub-G1 cells, and processing of multiple caspases and poly(ADP-ribose)polymerase cleavage. Pretreatment of cells with the specific mitogen-activated extracellular kinases (MEK) 1/2 inhibitor PD98059, together with 1f and 1o, resulted in an important enhancement of cell death, which might have clinical implications for the use of both compounds in combination with MEK 1/2 inhibitors as potential therapeutic agents. © 2012 Elsevier Masson SAS. All rights reserved.


De Armas P.,CSIC - Institute of Natural Products and Agrobiology | De Armas P.,Instituto Canario Of Investigacion Del Cancer | Tejedor D.,CSIC - Institute of Natural Products and Agrobiology | Tejedor D.,Instituto Canario Of Investigacion Del Cancer | And 2 more authors.
Angewandte Chemie - International Edition | Year: 2010

(Figure Presented) Simple and practical: The asymmetric alkynylation of imines has been revolutionized with two nice examples of a novel model of H-bonding asymmetric metal catalysis with Brønsted acids. The catalytic model comprises two well-differenti-ated and parallel catalytic cycles: one involving metallic alkynylydes (metal catalysis) and the other one using a chiral Brønsted acid (organocatalysis; see scheme; PG = protecting group). © 2010 Wiley-VCH Verlag GmbH S. Co. KGaA,.


Torres F.,University of Las Palmas de Gran Canaria | Torres F.,Instituto Canario Of Investigacion Del Cancer | Quintana J.,University of Las Palmas de Gran Canaria | Quintana J.,Instituto Canario Of Investigacion Del Cancer | And 2 more authors.
Molecular Carcinogenesis | Year: 2010

Flavonoids are polyphenolic compounds which display a vast array of biological activities and are promising anticancer agents. In this study we investigated the effect of 5,7,3′-trihydroxy-3,4′-dimethoxyflavone (THDF) on viability of nine human tumor cell lines and found that it was highly cytotoxic against leukemia cells. THDF induced G 2-M phase cell-cycle arrest and apoptosis through a caspase-dependent mechanism involving cytochrome c release, processing of multiple caspases (caspase-3, -6, -7, and -9) and cleavage of poly(ADP-ribose) polymerase. Overexpression of the protective mitochondrial proteins Bcl-2 and Bcl-x L conferred partial resistance to THDF-induced apoptosis. This flavonoid induced the phosphorylation of members of the mitogen-activated protein kinases (MAPKs) family and cell death was attenuated by inhibition of c-jun N-terminal kinases/stress-activated protein kinases (JNK/SAPK) and of extracellular signal-regulated kinases (ERK) 1/2. In the present study we report that THDF-induced cell death is mediated by an intrinsic dependent apoptotic event involving mitochondria and MAPKs, and through a mechanism independent of the generation of reactive oxygen species. The results suggest that THDF could be useful in the development of novel anticancer agents. © 2010 Wiley-Liss, Inc.

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