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281.
A Trifluorinated Thiazoline Scaffold Leading to Pro‐apoptotic Agents Targeting Prohibitins 下载免费PDF全文
Dr. Alba Pérez‐Perarnau Dr. Sara Preciado Dr. Claudia Mariela Palmeri Cristina Moncunill‐Massaguer Dr. Daniel Iglesias‐Serret Dr. Diana M. González‐Gironès Dr. Miriam Miguel Dr. Satoki Karasawa Dr. Satoshi Sakamoto Dr. Ana M. Cosialls Dr. Camila Rubio‐Patiño José Saura‐Esteller Dr. Rosario Ramón Dr. Laia Caja Dr. Isabel Fabregat Dr. Gabriel Pons Prof. Hiroshi Handa Prof. Fernando Albericio Prof. Joan Gil Prof. Rodolfo Lavilla 《Angewandte Chemie (International ed. in English)》2014,53(38):10150-10154
A new class of small molecules, with an unprecedented trifluorothiazoline scaffold, were synthesized and their pro‐apoptotic activity was evaluated. With an EC50 in the low micromolar range, these compounds proved to be potent inducers of apoptosis in a broad spectrum of tumor cell lines, regardless of the functional status of p53. Fast structure–activity relationship studies allowed the preparation of the strongest apoptosis‐inducing candidate. Using a high performance affinity purification approach, we identified prohibitins 1 and 2, key proteins involved in the maintenance of cell viability, as the targets for these compounds. 相似文献
282.
March R Pons J Ros J Clegg W Alvarez-Larena A Piniella JF Sanz J 《Inorganic chemistry》2003,42(23):7403-7409
The series of complexes [CdX(2)(C(5)H(4)NCOOR)] (X = Cl or Br; R = Me, Et, Pr(n)() or Pr(i)()) and [CdX(2)(C(5)H(4)NCOOR)(2)] (X = I; R = Me, Et, Pr(n)(), or Pr(i)()) have been obtained by the addition reaction of esters of 2-pyridinecarboxylic acid to cadmium(II) halides. X-ray crystal structures of two complexes [CdI(2)(C(5)H(4)NCOOR)(2)], R = Me (10) and R = Pr(n)() (12), have been determined. In both cases, the structure consists of discrete neutral monomeric units where the cadmium atom has a distorted octahedral coordination with CdI(2)N(2)O(2) core, two halides being in cis disposition. Structural information is compared with that deduced from (113)Cd CPMAS NMR experiments. Chemical shift anisotropies are discussed in terms of distortions produced in cadmium octahedra. The orientation of the principal axes of (113)Cd shielding tensor is also analyzed and related to the disposition of ligands in the structures of two analyzed compounds. 相似文献
283.
F. A. López M. C. Ramirez J. A. Pons A. López-Delgado F. J. Alguacil 《Journal of Thermal Analysis and Calorimetry》2008,94(2):517-522
This study presents an evaluation of the decomposition kinetic of low-grade nickeliferous laterite by thermogravimetric analysis.
Kinetic parameters were calculated using the Ozawa and the iso-conversional Friedman methods. Simplified kinetics models like
those based on the reaction order were also applied for the simulations. Two-dimensional shrinkage models of the reaction
interface mechanism were adopted as describing the thermal transformation process from non-isothermal kinetic analysis. The
iso-conversional method (model-free kinetics) reveals that the decomposition of low-grade nickeliferous laterite does not
follow a single mechanism because the determined activation energies and pre-exponential factor are not constant during the
course of the reaction. 相似文献