63254-88-6Relevant articles and documents
Tranylcypromine-Based LSD1 Inhibitors: Structure-Activity Relationships, Antiproliferative Effects in Leukemia, and Gene Target Modulation
Fioravanti, Rossella,Romanelli, Annalisa,Mautone, Nicola,Di Bello, Elisabetta,Rovere, Annarita,Corinti, Davide,Zwergel, Clemens,Valente, Sergio,Rotili, Dante,Botrugno, Oronza A.,Dessanti, Paola,Vultaggio, Stefania,Vianello, Paola,Cappa, Anna,Binda, Claudia,Mattevi, Andrea,Minucci, Saverio,Mercurio, Ciro,Varasi, Mario,Mai, Antonello
, p. 643 - 658 (2020/02/18)
Abstract: LSD1 is a lysine demethylase highly involved in initiation and development of cancer. To design highly effective covalent inhibitors, a strategy is to fill its large catalytic cleft by designing tranylcypromine (TCP) analogs decorated with long,
One-pot efficient synthesis of N α-urethane-protected β- And γ-amino acids
Cal, Marta,Jaremko, Mariusz,Jaremko, Lukasz,Stefanowicz, Piotr
, p. 1085 - 1091 (2013/07/05)
1-[(4-Methylphenyl)oxy]pyrrolidine-2,5-dione and 1-[(4-methylphenyl)oxy] piperidine-2,6-dione react in a Lossen-type reaction with primary alcohols in the presence of triethylamine to furnish corresponding N α- urethane-protected β-alanine and γ-aminopropionic acid (GABA), respectively, with excellent yields and purities, in an essentially "one-pot" procedure.
A phosgene and peroxide-free one-pot tandem synthesis of isatoic anhydrides involving anthranilic acid, boc anhydride and 2-chloro-N-methyl pyridinium iodide
Verma, Chhaya,Sharma, Somesh,Pathak, Arunendra
, p. 6897 - 6899 (2019/04/10)
A phosgene and peroxide-free approach for the synthesis of isatoic anhydrides has been described. The synthesis involves the carbamate formation with boc anhydride followed by in situ cyclization to afford the isatoic anhydride. The importance of this synthetic strategy is in the ease of operation, scalability and preparation from readily available raw materials.
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: Peptidomimetic replacement of the P2 amino acid by 2-aminoaryl acids and other non-natural amino acids
Wang, Yan,Jia, Shaojuan,Tseng, Ben,Drewe, John,Cai, Sui Xiong
, p. 6178 - 6182 (2008/04/02)
As a continuation of our SAR studies of dipeptidyl aspartyl-fmk as caspase inhibitors, we explored the replacement of the P2 amino acid by a 2-aminoaryl acid or other non-natural amino acids. Several of these compounds, such as 6l and 6p, were
Solid-phase combinatorial synthesis and cytotoxicity of 3-aryl-2,4-quinazolindiones
Park Choo, Hea-Young,Kim, Mihyun,Lee, Sang Kook,Woong Kim, Sang,Kwon Chung, In
, p. 517 - 523 (2007/10/03)
A series of 3-aryl-2,4-quinazolinediones with various substitution on aromatic rings has been prepared by solid-phase synthesis. Several compounds showed cytotoxicity on human colon carcinoma (Col2) tested by SRB method.
Direct conversion of azides to carbamates and sulfonamides using Fe/NH4Cl: Effect of sonication
Chandrasekhar,Narsihmulu
, p. 7969 - 7972 (2007/10/03)
A simple, direct and effective conversion of azides to carbamates and sulfonamides is achieved using Fe/NH4Cl in methanol. The influence of sonication and direct application in solution phase combinatorial chemistry are also studied by developing a 6x4 matrix library. (C) 2000 Elsevier Science Ltd.
Studies on 2-benzyloxy-4H-3,1-benzoxazin-4-ones as serine protease inhibitors
Guetschow, Michael,Neumann, Ulf,Sieler, Joachim,Eger, Kurt
, p. 95 - 103 (2007/10/03)
The class of 3,1-benzoxazin-4-ones includes potent inhibitors of various serine proteases. Structural investigations on three 2-benyloxy-4H-3,1-benzoxazin-4-ones (1-3) are described with respect to their reactivity to alkaline hydrolysis. The 13/sup
Synthesis of cyclic depsipeptides and peptides via direct amide cyclization
Villalgordo, Jose M.,Heimgartner, Heinz
, p. 748 - 766 (2007/10/03)
The 2,2-disubstituted 2H-azirin-3-amines 7 (2,2-disubstituted 3-amino-2H-azirines) were used as amino-acid synthons in the preparation of medium-sized cyclic depsipeptides and peptides derived from salicylic acids 6 and anthranilic acid 19, respectively.
Inhibition of cathepsin G by 4H-3,1-benzoxazin-4-ones
Guetschow, Michael,Neumann, Uf
, p. 1935 - 1942 (2007/10/03)
A series of 4H-3,1-benzoxazin-4-ones is reported that inhibit the serine proteases human cathepsin G and bovine chymotrypsin. The synthesis and kinetic parameters of the alkaline hydrolysis is described. These compounds act as acyl-enzyme inhibitors of bo
