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Aginagalde M.,University of the Basque Country | Vara Y.,IkerChem | Arrieta A.,University of the Basque Country | Zangi R.,University of the Basque Country | And 4 more authors.
Journal of Organic Chemistry | Year: 2010

The reaction between benzynes and imidazo[1,2-a]pyridines (pyrimidines) to form benzo[a]imidazo[5,1,2-cd]indolizines and 2,3,9c-triazocyclopenta[j,k] fluorenes has been studied computationally and experimentally. It is found that these reactions take place via tandem [ π8 s + π2 s] and [ -2 s + π6 s + -2 s] processes. The [8 + 2] cycloaddition steps are essentially barrierless, and the aromatization steps occur via highly synchronous aromatic transition structures. From an experimental standpoint, the reaction is feasible under microwave irradiation and using 2-(trimethylsilyl)phenyl triflates as benzyne precursors. Depending on the substitution pattern in the starting triflate a complete regiocontrol of the reaction can be achieved. The tetracyclic compounds thus prepared emitted blue light when excited at 365 nm and exhibited interesting photophysical properties. © 2009 American Chemical Society. Source

Arias L.,University of the Basque Country | Vara Y.,IkerChem | Cossio F.P.,University of the Basque Country
Journal of Organic Chemistry | Year: 2012

In this paper, a fully regiocontrolled synthesis of either 2- and 3-substituted benzo[b]furans is described. Direct reaction between phenols and α-bromoacetophenones in the presence of neutral alumina yields 2-substituted benzo[b]furans with complete regiocontrol. When a basic salt such as potassium carbonate is used, the corresponding 2-oxoether is obtained. Cyclization of these latter compounds promoted by neutral alumina yields the corresponding 3-substituted benzo[b]furans. Using the former method, Moracin M and other analogues can be obtained from commercial sources in two preparative steps. DFT calculations provide reasonable reaction paths to understand the formation of 2-substituted benzo[b]furans. © 2011 American Chemical Society. Source

Aginagalde M.,University of the Basque Country | Gomez-Vallejo V.,CIC Biomagune | Vara Y.,IkerChem | Cossio F.P.,University of the Basque Country | Llop J.,CIC Biomagune
Applied Radiation and Isotopes | Year: 2012

In the present paper, the synthesis of 11C-labeled Kendine 91 (a HDAC inhibitor which has shown in vitro and in vivo activity in HCT 116 and MOLT 4 human cancer cell lines) is described for the first time. The radiosynthesis has been approached by reaction of the non-radioactive precursor 6-((3-(4-hydroxyphenyl)-5-phenyl-1H-pyrrole-2-carboxamide))hexanehydroxamic acid with [ 11C]CH 3I in basic media. Despite the presence of more than one reactive site in the chemical structure of the precursor, acceptable radiochemical yield (8.2±2.1%, decay corrected to the end of bombardment), specific activity (28.2±9.4GBq/μmol) and radiochemical purity values (>95%) were obtained in reasonably short preparation times (~40min). Despite the moderate radiochemical yield, final radioactivity and radioactivity concentration values (1.8±0.3GBq and 180MBq/ml, respectively) should be sufficient for putative in vivo studies in animals. © 2012 Elsevier Ltd. Source

Zubia-Olascoaga A.,IkerChem | Bujanda L.,University of the Basque Country
World Journal of Gastroenterology | Year: 2012

Pancreatic cancer is the deadliest solid cancer and currently the fourth most frequent cause of cancer-related deaths. Emerging evidence suggests that cancer stem cells (CSCs) play a crucial role in the development and progression of this disease. The identification of CSC markers could lead to the development of new therapeutic targets. In this study, the authors explore the functional role of c-Met in pancreatic CSCs, by analyzing self-renewal with sphere assays and tumorigenicity capacity in NOD SCID mice. They concluded that c-Met is a novel marker for identifying pancreatic CSCs and c-Methigh in a higher tumorigenic cancer cell population. Inhibition of c-Met with XL184 blocks self-renewal capacity in pancreatic CSCs. In pancreatic tumors established in NOD SCID mice, c-Met inhibition slowed tumor growth and reduced the population of CSCs, along with preventing the development of metastases. © 2012 Baishideng. All rights reserved. Source

The present invention refers to compounds of formula (I): as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or chemoprevention of cancer hematological malignancy, proliferative diseases, genetic diseases, neurological disorders and immunological disorders.

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