86770-47-0Relevant academic research and scientific papers
Transformation of the non-selective aminocyclohexanol-based Hsp90 inhibitor into a Grp94-seletive scaffold
Mishra, Sanket J.,Ghosh, Suman,Stothert, Andrew R.,Dickey, Chad A.,Blagg, Brian S. J.
, p. 244 - 253 (2017/12/30)
Glucose regulated protein 94 kDa, Grp94, is the endoplasmic reticulum (ER) localized isoform of heat shock protein 90 (Hsp90) that is responsible for the trafficking and maturation of toll-like receptors, immunoglobulins, and integrins. As a result, Grp94 has emerged as a therapeutic target to disrupt cellular communication, adhesion, and tumor proliferation, potentially with fewer side effects compared to pan-inhibitors of all Hsp90 isoforms. Although, the N-terminal ATP binding site is highly conserved among all four Hsp90 isoforms, recent cocrystal structures of Grp94 have revealed subtle differences between Grp94 and other Hsp90 isoforms that has been exploited for the development of Grp94-selective inhibitors. In the current study, a structure-based approach has been applied to a Grp94 nonselective compound, SNX 2112, which led to the development of 8j (ACO1), a Grp94-selective inhibitor that manifests -440 nM affinity and ≥200-fold selectivity against cytosolic Hsp90 isoforms.
An efficient one-pot synthesis of 2-benzylpyrroles and 3-benzylindoles
Sharma, Ratnesh,Chouhan, Mangilal,Sood, Divya,Nair, Vipin A.
experimental part, p. 305 - 309 (2012/01/03)
One-pot regioselective benzylation of pyrroles and indoles using zirconium tetrachloride is discussed. This has been achieved by in-situ generation of di(1H-pyrrol-1-yl)zirconium(IV) chloride and di(1H-indol-1-yl)zirconium(IV) chloride. It was observed th
A General Method for the Preparation of 2-Benzylpyrroles by Modified Borohydride Reduction of Azafulvenium Salts
McGillivray, George,Smal, Elma
, p. 633 - 636 (2007/10/02)
2-Benzylpyrroles (5a-h) can be prepared in high yield from pyrroles by reduction, with modified borohydride reagents, of the corresponding 1-azafulvenium salts (3a-h) generated in situ in the presence of excess of phosphoryl trichloride.The procedure is compatible with ester groups.
2-(Nuclearly-substituted)benzylpyrrolidines
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, (2015/02/20)
2-Benzylpyrrolidines bearing from 1 to 4 nuclear substituents on the benzyl ring are pharmacologically active, particularly on the CNS, on blood pressure and on pain sensation for warm-blooded animals. They are synthesized, e.g., by reducing appropriate 2-benzylpyrrolidines and are formulated into medicament compositions according to established conventional techniques.
