333382-87-9Relevant academic research and scientific papers
POLYCYCLIC COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES
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Paragraph 1524; 1525, (2020/03/29)
The present disclosure relates to bifunctional compounds, ULM— L—PTM, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A- RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
Liquid crystalline paracyclophanes and ansa compounds - Series of polyether macrocycles incorporating diacetylene, phenyl, biphenyl, p-terphenyl and 2,5-diphenyl-1,3,4-thiadiazole rigid cores
Hegmann, Torsten,Neumann, Bernhard,Wolf, Raik,Tschierske, Carsten
, p. 1025 - 1034 (2007/10/03)
Series of different macrocyclic liquid crystals consisting of two rod-like aromatic cores connected at both terminal ends by polyether chains have been synthesised by various macrocyclisation reactions (template assisted etherification, Yamaguchi macrolactonisation, Glaser-coupling reaction). The nature and length of the rigid core have a dominant impact on the liquid crystalline phases formed. A stepwise increase of the length of one of the rigid cores leads to significant mesophase stabilisation, to the induction of lamellar phases and, in general, to wider mesophase ranges. The same types of mesophases but at much reduced transition temperatures are observed when flexible methylene linkages are incorporated into the macrocycles. Parallel pre-organisation of the calamitic cores and micro-segregation of chemically distinct molecular parts are discussed as the main driving forces for the mesophase behaviour of these macrocyclic compounds. Additionally, chiral macrocyclic liquid crystals exhibiting SmC* phases, cholesteric phases and blue phases have been synthesised. In contrast to the cyclophanes, ansa-compounds incorporating only one aromatic core within the macrocycle show either a monotropic nematic phase only or no liquid crystalline behaviour at all. An architecture combining the cyclophane structure with an ansa-unit and a molecule with a non-parallel pre-organisation of rod-like mesogenic cores as well does not show LC phases. The lack of LC behaviour for these compounds might be due to the molecular architecture resulting in a steric disturbance of packing that, in this way, does not allow for segregation of rigid and flexible units into distinct sub-domains. The Royal Society of Chemistry 2005.
Synthesis of pyridinocrownophanes exhibiting high Ag+-affinity
Inokuma, Seiichi,Kimura, Koichi,Funaki, Takashi,Nishimura, Jun
, p. 123 - 130 (2007/10/03)
Crownophanes possessing a pyridine moiety were prepared by means of intramolecular [2 + 2] photocycloaddition of the styrene derivatives. The crown compounds having six to ten ethereal oxygens selectively extracted Ag+ with high efficiency in the liquid-liquid extraction. The high extractability and efficiency were maintained even at low pH region of the extraction system. From ESI-MS analysis, it was found that the crownophanes formed some kinds of complexes having 1:1 and 2:1 stoichiometry (host/guest) with Ag+ and Pb2+ in MeCN-H2O homogeneous system.
SELECTIV BROMINATION OF THE AROMATIC RING IN ω-PHENYLPOLYOXAALKANES AND ALKANOLS IN MICELLES
Jursic, Branko
, p. 1553 - 1558 (2007/10/02)
The regioselecticity of bromination of ω-phenylpolyoxaalkanes and alkanols by bromine in aqueous solution of dodecyl sulfate (SDS) and aqueous solution of cetyltrimethylammonium bromide (CTAB) are shown to be related to the average orientation of substrate as indicated by 1H NMR studies.Thus ortho-bromination is promoted at higher concentrations of the surfactant relative to pure water.In contrast, at an equal ratio of the surfactant and substrate para-bromination is promoted.The results are discussed with respect to the average orientation of substrate in a micellar microenvironment and the formation of an ether-bromine comples as possible bromination agent.
