5783-36-8Relevant articles and documents
A Novel Biphenyl-based Chemotype of Retinoid X Receptor Ligands Enables Subtype and Heterodimer Preferences
Pollinger, Julius,Schierle, Simone,Gellrich, Leonie,Ohrndorf, Julia,Kaiser, Astrid,Heitel, Pascal,Chaikuad, Apirat,Knapp, Stefan,Merk, Daniel
supporting information, p. 1346 - 1352 (2019/09/12)
The nuclear retinoid X receptors (RXRs) are key ligand sensing transcription factors that serve as universal nuclear receptor heterodimer partners and are thus involved in numerous physiological processes. Therapeutic targeting of RXRs holds high potential but available RXR activators suffer from limited safety. Selectivity for RXR subtypes or for certain RXR heterodimers are promising strategies for safer RXR modulation. Here, we report systematic structure-activity relationship studies on biphenyl carboxylates as new RXR ligand chemotype. We discovered specific structural modifications that enhance potency on RXRs, govern subtype preference, and vary modulation of different RXR heterodimers. Fusion of these structural motifs enabled specific tuning of subtype preferential profiles with markedly improved potency. Our results provide further evidence that RXR subtype selective ligands can be designed and present a novel chemotype of RXR modulators that can be tuned for subtype and heterodimer preferences.
Synthesis and study of the catalytic applications in C–C coupling reactions of hybrid nanosystems based on alumina and palladium nanoparticles
Hossain, Abul Monsur Showkot,Balbín, Adriana,Erami, Roghayeh Sadeghi,Prashar, Sanjiv,Fajardo, Mariano,Gómez-Ruiz, Santiago
, p. 645 - 652 (2016/12/09)
Nanostructured alumina has been treated under mild conditions with different quantities of [PdCl2(cod)] (cod = 1,5-cyclooctadiene) to promote the formation of supported palladium nanoparticles which have been characterized by XRD, XRF, BET and TEM. The results show that the new hybrid materials, nano-Al2O3-Pd-20 and nano-Al2O3-Pd-50, consist of impregnated palladium nanoparticles onto aggregates of nanoparticles of alumina. The catalytic activity of the hybrid Pd-alumina materials has been tested in Suzuki–Miyaura C–C coupling reactions observing good conversion rates in the reactions of 3-bromoanisole with 4-carboxyphenylboronic acid or 4-vinylphenylboronic acid. The catalytic studies have been extended with experiments investigating the Pd loading influence. Catalyst recyclability tests show a slight decrease in activity after the first cycle in the reaction of 3-bromoanisole with 4-vinylphenylboronic acid. However, subsequent activity remains almost constant after five more consecutive catalytic cycles.
Dual application of Pd nanoparticles supported on mesoporous silica SBA-15 and MSU-2: Supported catalysts for C-C coupling reactions and cytotoxic agents against human cancer cell lines
Balbn, Adriana,Gaballo, Francesco,Ceballos-Torres, Jess,Prashar, Sanjiv,Fajardo, Mariano,Kaluderovi, Goran N.,Gmez-Ruiz, Santiago
, p. 54775 - 54787 (2015/02/02)
Two different mesoporous silica-based materials (SBA-15 and MSU-2) have been treated under mild conditions with different quantities of [PdCl2(cod)] (cod = 1,5-cyclooctadiene) to promote the formation of supported palladium nanoparticles (materials of the type SBA-15-Pd and MSU-2-Pd). The synthesized materials have been characterized by different techniques observing that the palladium nanoparticles remain impregnated in the silica. The catalytic activity of the hybrid Pd-silica materials has been tested in Suzuki-Miyaura C-C coupling reactions observing moderate conversion rates in the reactions of 3-bromoanisole with 4-carboxyphenylboronic acid and 2-bromopyridine with 4-carboxyphenylboronic acid. In addition, the synthesized materials showed a good degree of recyclability, being catalytically active in five consecutive catalytic tests. Finally, in order to evaluate the cytotoxicity of the synthesized materials, in vitro tests against five different human cancer cell lines have been carried out, observing high cytotoxic activities of the hybrid systems comparable if not somewhat higher to other systems based on metal complexes supported on mesoporous silicas described previously in the literature. To the best of our knowledge the cytotoxic study reported here represents the first evaluation of the anticancer action of supported palladium nanoparticles in human cancer cells.
