81396-84-1Relevant academic research and scientific papers
Harnessing Additional Capability from in Water Reaction Conditions: Aldol versus Knoevenagel Chemoselectivity
Ali El Damrany Hussein, Hussein,Debnath, Samarpita,Goswami, Falguni,Hussain, Ishtiaq,Karn, Alka,Nakka, Srinuvasu,Nugent, Thomas C.
supporting information, p. 3539 - 3545 (2021/06/12)
Aldol reaction chemoselectivity, racemic or enantioselective, has not been previously demonstrated in the presence of Knoevenagel active functional groups. Here, we show that unhindered β-diketones remain unreacted while a ketone moiety undergoes a highly
Unveiling epidithiodiketopiperazine as a non-histone arginine methyltransferase inhibitor by chemical protein methylome analyses
Sohtome, Yoshihiro,Shimazu, Tadahiro,Barjau, Joaquin,Fujishiro, Shinya,Akakabe, Mai,Terayama, Naoki,Dodo, Kosuke,Ito, Akihiro,Yoshida, Minoru,Shinkai, Yoichi,Sodeoka, Mikiko
supporting information, p. 9202 - 9205 (2018/08/24)
We present a chemical methylome analysis platform to evaluate the inhibitory activity of small molecules towards poorly characterized protein methyltransferases (PMTs), facsilitating to identify syn-HyPA-ETP-2 as a non-histone arginine methyltransferase inhibitor.
Compound as apoptosis protein inhibitor, and application thereof
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Paragraph 0116; 0118; 0119; 0120, (2018/09/12)
The present invention belongs to the field of medical chemistry, relates to a class of compounds of apoptosis protein inhibitors, and applications thereof, and particularly provides a compound represented by a formula I, or an isomer thereof, a pharmaceut
Design, Synthesis, and Biological Evaluation of Peptidomimetic N-Substituted Cbz-4-Hyp-Hpa-Amides as Novel Inhibitors of Plasmodium falciparum
Bacherikov, Valeriy A.,Chittiboyina, Amar G.,Avery, Mitchell A.
, (2017/08/18)
A new series of peptidomimetic N-substituted Cbz-4-Hyp-Hpa-amides were designed, synthesized, and evaluated for inhibition of the Plasmodium falciparum. Substituents on the N-atom of the amide group were selected alkyl-, allyl-, aryl-, 2-hydroxyethyl-, 2-
Process Development and Synthesis of Birinapant: Large Scale Preparation and Acid-Mediated Dimerization of the Key Indole Intermediate
Deng, Yijun,Xie, Qiuzhe,LaPorte, Matthew G.,Chasnoff, Anna T. A.,Mortensen, Mark A.,Patra, Debasis,Putrelo, Seth A.,Antonovich, Robert S.,Cao, Hong,Yan, Jun,Cooper, Arthur J.,Rippin, Susan R.,Alexander, Matthew D.,Kumar, Pavan Tirunahari,Hendi, Mukta S.,Lee, Yu-Hua,Haimowitz, Thomas,Condon, Stephen M.
, p. 242 - 252 (2016/03/04)
Birinapant/TL32711 (1) is a novel bivalent antagonist of the inhibitor of apoptosis (IAP) family of proteins which is currently in clinical development for the treatment of cancer and hepatitis B virus (HBV) infection. In this report, we present a detaile
SMAC MIMETIC (BIRINAPANT) FOR USE IN THE TREATMENT OF PROLIFERATIVE DISEASES (CANCER)
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Paragraph 0055; 0056, (2013/04/13)
A method of using a Smac mimetic and pharmaceutical compositions thereof.
Asymmetric Mannich reactions catalyzed by proline and 4-hydroxyproline derived organocatalysts in the presence of water
Veverkova, Eva,Liptakova, Lucia,Veverka, Miroslav,Sebesta, Radovan
, p. 548 - 552 (2013/06/27)
The ability of amphiphilic catalysts based on proline and 4-hydroxyproline to catalyze the Mannich reaction in aqueous media is reported. With a 4-tert-butyldimethylsiloxy-substituted organocatalyst derived from N-prolylsulfonamide, the reaction of cyclohexanone with iminoglyoxylate proceeds with high enantioselectivity (>99% ee for the syn-diastereomer). This catalyst was also successfully applied in a reaction of an iminoglyoxylate with an aqueous tetrahydro-2H-pyran-2,6-diol to give the corresponding 2,3-disubstituted tetrahydropyridine with up to 95:5 dr and 98% ee.
SMAC Mimetic
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Page/Page column 7, (2011/01/12)
A SMAC mimetic and pharmaceutical compositions thereof and methods of use.
IAP INHIBITORS
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Page/Page column 76-77, (2009/09/05)
The present invention describes compounds of the following formula: processes for their preparation, pharmaceutical compositions containing them, and their use in therapy. The compounds of the present invention inhibit IAPs (inhibitors of apoptosis protei
A simple synthesis of 4-substituted 2-(3-hydroxy-2-oxo-1-phenethyl- propylcarbamoyl)pyrrolidine-1-carboxylic acid benzyl esters as novel cysteine protease inhibitors
Oh, Seikwan,Jung, Jae-Chul
experimental part, p. 210 - 216 (2008/10/09)
A convenient synthesis of 4-substituted 2-(3-hydroxy-2-oxo-1- phenethylpropylcarbamoyl)pyrrolidine-1-carboxylic acid benzyl esters 17 and 18 as new cysteine protease inhibitors is described. The synthetic key strategies involve the diazocarbonyl insertion
