401573-23-7Relevant academic research and scientific papers
INHIBITORS OF THE MENIN-MLL INTERACTION
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Page/Page column 347, (2018/01/17)
The present invention is directed to inhibitors of the interaction of menin with MLL and MLL fusion proteins, pharmaceutical compositions containing the same, and their use in the treatment of cancer and other diseases mediated by the menin-MLL interaction.
Synthesis and application of a new fluorous-tagged ammonia equivalent
Nielsen, Simon D.,Smith, Garrick,Begtrup, Mikael,Kristensen, Jesper L.
supporting information; experimental part, p. 4557 - 4566 (2010/08/20)
A novel fluorous-tagged ammonia equivalent has been developed. It is based on a nitrogen-oxygen bond, which can be cleaved in a traceless manner by a molybdenum complex or samarium diiodide. The application in the synthesis of ureas, amides, sulfonamides, and carbamates is described. The scope of the fluo-rous N-O linker is exemplified by the synthesis of itopride, a drug used for the treatment of functional dyspepsia. Itopride was synthesized with the aid of fluorous purification methods and the product was isolated in good overall yield, with high purity.
Improved syntheses of 5′- S -(2-Aminoethyl)-6- N -(4-nitrobenzyl)- 5′-thioadenosine (SAENTA), analogues, and fluorescent probe conjugates: Analysis of cell-surface human equilibrative nucleoside transporter 1 (hENT1) levels for prediction of the antitumor
Robins, Morris J.,Peng, Yunshan,Damaraju, Vijaya L.,Mowles, Delores,Barron, Geraldine,Tackaberry, Tracey,Young, James D.,Cass, Carol E.
experimental part, p. 6040 - 6053 (2010/11/02)
5′-S-(2-Aminoethyl)-6-N-(4-nitrobenzyl)-5′-thioadenosine (SAENTA), 5′-S-(2-acetamidoethyl)-6-N-[(4-substituted)benzyl]-5′- thioadenosine analogues, 5′-S-[2-(6-aminohexanamido)]ethyl-6-N-(4- nitrobenzyl)-5′-thioadenosine (SAHENTA), and related compounds we
N-(3-acyloxy-2-benzylpropyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues: Novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor
Lee, Jeewoo,Lee, Jiyoun,Kang, Myungshim,Shin, Myoungyoup,Kim, Ji-Min,Kang, Sang-Uk,Lim, Ju-Ok,Choi, Hyun-Kyung,Suh, Young-Ger,Park, Hyeung-Geun,Oh, Uhtaek,Kim, Hee-Doo,Park, Young-Ho,Ha, Hee-Jin,Kim, Young-Ho,Toth, Attila,Wang, Yun,Tran, Richard,Pearce, Larry V.,Lundberg, Daniel J.,Blumberg, Peter M.
, p. 3116 - 3126 (2007/10/03)
Isosteric replacement of the phenolic hydroxyl group in potent vanilloid receptor (VR1) agonists with the alkylsulfonamido group provides a series of compounds which are effective antagonists to the action of the capsaicin on rat VR1 heterologously expressed in Chinese hamster ovary (CHO) cells. In particular, compound 61, N-[2-(3,4-dimethylbenzyl)-3-pivaloyloxypropyl]-N′-[3-fluoro-4- (methylsulfonylamino)benzyl]thiourea was a full antagonist against capsaicin, displayed a Ki value of 7.8 nM (compared to 520 nM for capsazepine and 4 nM for 5-iodoRTX), and showed excellent analgesic activity in mice. Structure-activity analysis of the influence of modifications in the A- and C-regions of 4-methylsulfonamide ligands on VR1 agonism/antagonism indicated that 3-fluoro substitution in the A-region and a 4-tert-butylbenzyl moiety in the C-region favored antagonism, whereas a 3-methoxy group in the A-region and 3-acyloxy2-benzylpropyl moieties in the C-region favored agonism.
