59604-96-5Relevant academic research and scientific papers
A Domino Diels-Alder Approach toward the Tetracyclic Nicandrenone Framework
MacKay, Emily G.,N?rret, Marck,Wong, Leon S.-M.,Louis, Ignace,Lawrence, Andrew L.,Willis, Anthony C.,Sherburn, Michael S.
supporting information, p. 5517 - 5519 (2015/12/23)
The tetracarbocyclic framework of the nicandrenone natural products is formed in one step from a linear precursor via a domino intramolecular Diels-Alder/intramolecular furan Diels-Alder/aromatization sequence. The approach represents a new 0 → ABCD strategy for the preparation of aromatic steroids.
TETRAZOLE COMPOUNDS AND METHODS OF MAKING AND USING SAME
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Page/Page column 52, (2012/08/08)
Described herein are tetrazole compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tetrazole compounds are provided. The compounds are contemplated to have activity against meth
Synthesis of bicyclic salicylates by [3+3] cyclization of 1,3-bis(silyl enol ethers) with cyclic 3-(silyloxy)alk-2-en-1-ones
H?tteckea, Nicole,Reinkea, Helmut,Fischerb, Christine,Langera, Peter
experimental part, p. 699 - 706 (2009/12/26)
Bicyclic salicylates were prepared by [3+3] cyclization of 1,3-bis(silyl enol ethers) with cyclic 3-(silyloxy)alk-2-en-1-ones.
Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: A structural basis for the reduction of albumin binding
Sheppard, George S.,Wang, Jieyi,Kawai, Megumi,Fidanze, Steve D.,BaMaung, Nwe Y.,Erickson, Scott A.,Barnes, David M.,Tedrow, Jason S.,Kolaczkowski, Lawrence,Vasudevan, Anil,Park, David C.,Wang, Gary T.,Sanders, William J.,Mantei, Robert A.,Palazzo, Fabio,Tucker-Garcia, Lora,Lou, Pingping,Zhang, Qian,Park, Chang H.,Kim, Ki H.,Petros, Andrew,Olejniczak, Edward,Nettesheim, David,Hajduk, Phillip,Henkin, Jack,Lesniewski, Richard,Davidsen, Steven K.,Bell, Randy L.
, p. 3832 - 3849 (2007/10/03)
Methionine aminopeptidase-2 (MetAP2) is a novel target for cancer therapy. As part of an effort to discover orally active reversible inhibitors of MetAP2, a series of anthranilic acid sulfonamides with micromolar affinities for human MetAP2 were identified using affinity selection by mass spectrometry (ASMS) screening. These micromolar hits were rapidly improved to nanomolar leads on the basis of insights from protein crystallography; however, the compounds displayed extensive binding to human serum albumin and had limited activity in cellular assays. Modifications based on structural information on the binding of lead compounds to both MetAP2 and domain III of albumin allowed the identification of compounds with significant improvements in both parameters, which showed good cellular activity in both proliferation and methionine processing assays.
Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties
Kawai, Megumi,BaMaung, Nwe Y.,Fidanze, Steve D.,Erickson, Scott A.,Tedrow, Jason S.,Sanders, William J.,Vasudevan, Anil,Park, Chang,Hutchins, Charles,Comess, Kenneth M.,Kalvin, Douglas,Wang, Jieyi,Zhang, Qian,Lou, Pingping,Tucker-Garcia, Lora,Bouska, Jennifer,Bell, Randy L.,Lesniewski, Richard,Henkin, Jack,Sheppard, George S.
, p. 3574 - 3577 (2007/10/03)
We have screened molecules for inhibition of MetAP2 as a novel approach toward antiangiogenesis and anticancer therapy using affinity selection/mass spectrometry (ASMS) employing MetAP2 loaded with Mn2+ as the active site metal. After a series
A Novel Cycloaromatization Reaction. Regiocontrolled Synthesis of Substituted Methyl Salicylates
Chan, Tak-Hang,Brownbridge, Peter
, p. 3534 - 3538 (2007/10/02)
A new method of constructing six-membered rings, involving the condensation of two three-carbon units, one with two nucleophilic sites and the other containing two electrophilic sites, is reported.The regiochemistry of the reaction is controlled by the differential reactivities of these sites. 1,3-Bis(trimethylsiloxy)-1-methoxybuta-1,3-diene (1) constitutes the three-carbon fragment with two nucleophilic sites.Condensation of 1 with various equivalents of β-dicarbonyl compounds and titanium tetrachloride gave substituted methyl salicylates.The regiochemistry is controlled by the order of reactivity of the electrophilic sites, which is conjugate position of enone > ketone > monothioacetal, acetal.
AMINOTETRALOLS
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, (2008/06/13)
Novel aminotetralol compounds of the formula STR1 wherein R 1 is hydrogen, acyl derived from carboxylic acid, or a hydrocarbon group which may be substituted;--OZ 1 is hydroxyl which may be protected; Y is hydrogen, acyl, hydroxyl which may be protected,
