6885-44-5Relevant articles and documents
CORTISTATIN ANALOGUES AND SYNTHESES AND USES THEREOF
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, (2015/07/15)
Provided herein are compounds of Formula (A), (B), (C), (D) and (E), pharmaceutically acceptable salts, quaternary amine salts, and N-oxides thereof, and pharmaceutical compositions thereof. Compounds of Formula (A), (B), (C), (D), and (E) are contemplated useful as therapeutics for treating a wide variety of conditions, e.g., including but not limited to, conditions associated with angiogenesis and with CDK8 and/or CDK19 kinase activity. Further provided are methods of inhibiting CDK8 and/or CDK19 kinase activity, methods of modulating the β-catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGFβ/BMP pathway, methods of modulating HIF-1 -alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using a compound of Formula (A), (B), (C), (D), or (E). Further provided are CDK8 and CDK19 point mutants and methods of use thereof.
Total synthesis with a chirogenic opening move demonstrated on steroids with estrane or 18a-homoestrane skeleton
Quinkert,Del Grosso,Doring,Doring,Schenkel,Bauch,Dambacher,Bats,Zimmermann,Durner
, p. 1345 - 1391 (2007/10/02)
A concept of first choice for the synthesis of the title compounds had been proposed by Dane in the late 1930s. It was soon turned down, because the opening move - a chirogenic Diels-Alder reaction - did not work. With Lewis acids as mediators, however, a successful start has been achieved now. With Ti complexes of chelating ligands (Seebach's TADDOLs (= α,α,α',α'-tetraaryl-1,3-dioxolane-4,5-dimethanols)), enantioselective formation of the desired adducts does occur. Efficient total syntheses of 2 and 3a have been accomplished.
Highly selective total synthesis of 19-nor-steroids via a photochemical key reaction: Racemic target compounds
Quinkert,Weber,Schwartz,et al.
, p. 2335 - 2371 (2007/10/02)
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