173989-76-9Relevant articles and documents
Structure-activity relationship and liver microsome stability studies of pyrrole necroptosis inhibitors
Teng, Xin,Keys, Heather,Yuan, Junying,Degterev, Alexei,Cuny, Gregory D.
body text, p. 3219 - 3223 (2009/04/06)
Necroptosis is a regulated caspase-independent cell death pathway resulting in morphology reminiscent of passive non-regulated necrosis. Several diverse structure classes of necroptosis inhibitors have been reported to date, including a series of [1,2,3]thiadiazole benzylamide derivatives. However, initial evaluation of mouse liver microsome stability indicated that this series of compounds was rapidly degraded. A structure-activity relationship (SAR) study of the [1,2,3]thiadiazole benzylamide series revealed that increased mouse liver microsome stability and increased necroptosis inhibitory activity could be accomplished by replacement of the 4-cyclopropyl-[1,2,3]thiadiazole with a 5-cyano-1-methylpyrrole. In addition, the SAR and the cellular activity profiles, utilizing different cell types and necroptosis-inducing stimuli, of representative [1,2,3]thiadiazole and pyrrole derivatives were very similar suggesting that the two compound series inhibit necroptosis in the same manner.
Asymmetric rhodium carbene insertion into the Si-H bond: Identification of new dirhodium(II) carboxylate catalysts using parallel synthesis techniques
Buck, Richard T.,Coe, Diane M.,Drysdale, Martin J.,Ferris, Leigh,Haigh, David,Moody, Christopher J.,Pearson, Neil D.,Sanghera, J. Bobby
, p. 791 - 816 (2007/10/03)
Decomposition of methyl 2-diazophenylacetate in the presence of silanes and a chiral dirhodium(II) catalyst results in Si-H insertion of the intermediate carbenoid with varying degrees of enantioselectivity. New chiral dirhodium(II) carboxylate catalysts were identified using solution phase parallel synthesis techniques.
New chiral rhodium(II) carboxylates and their use as catalysts in carbenoid transformations
Ferris, Leigh,Haigh, David,Moody, Christopher J.
, p. 107 - 110 (2007/10/02)
New chiral dirhodium(II) carboxylates 11-15 have been prepared from the half phthalate esters 6-8 and the pyrroles 9 and 10, and their use as catalysts for the decomposition of diazocarbonyl compounds 16 and 18 investigated.