52200-49-4Relevant articles and documents
COMPOUNDS AND USES THEREOF
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Page/Page column 71; 123, (2021/08/06)
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
Development of novel selective peptidomimetics containing a boronic acid moiety, targeting the 20s proteasome as anticancer agents
Scarbaci, Kety,Troiano, Valeria,Ettari, Roberta,Pinto, Andrea,Micale, Nicola,Di Giovanni, Carmen,Cerchia, Carmen,Schirmeister, Tanja,Novellino, Ettore,Lavecchia, Antonio,Zappalà, Maria,Grasso, Silvana
, p. 1801 - 1816 (2014/08/18)
This paper describes the design, synthesis, and biological evaluation of peptidomimetic boronates as inhibitors of the 20S proteasome, a validated target in the treatment of multiple myeloma. The synthesized compounds showed a good inhibitory profile against the ChT-L activity of 20S proteasome. Compounds bearing a β-alanine residue at the P2 position were the most active, that is, 3-ethylphenylamino and 4-methoxyphenylamino (R)-1-{3-[4-(substituted)-2- oxopyridin-1(2H)-yl]propanamido}-3-methylbutylboronic acids (3 c and 3 d, respectively), and these derivatives showed inhibition constants (Ki) of 17 and 20 nM, respectively. In addition, they co-inhibited post glutamyl peptide hydrolase activity (3 c, Ki=2.57 μM; 3 d, K i=3.81 μM). No inhibition was recorded against the bovine pancreatic α-chymotrypsin, which thus confirms the selectivity towards the target enzyme. Docking studies of 3 c and related inhibitors into the yeast proteasome revealed the structural basis for specificity. The evaluation of growth inhibitory effects against 60 human tumor cell lines was performed at the US National Cancer Institute. Among the selected compounds, 3 c showed 50 % growth inhibition (GI50) values at the sub-micromolar level on all cell lines.
Synthesis and SAR studies of novel heteroaryl fused tetracyclic indole-diamide compounds: Potent allosteric inhibitors of the hepatitis C virus NS5B polymerase
Ding, Min,He, Feng,Hudyma, Thomas W.,Zheng, Xiaofan,Poss, Michael A.,Kadow, John F.,Beno, Brett R.,Rigat, Karen L.,Wang, Ying-Kai,Fridell, Robert A.,Lemm, Julie A.,Qiu, Dike,Liu, Mengping,Voss, Stacey,Pelosi, Lenore A.,Roberts, Susan B.,Gao, Min,Knipe, Jay,Gentles, Robert G.
scheme or table, p. 2866 - 2871 (2012/05/20)
Presented here are initial structure-activity relationship (SAR) studies on a series of novel heteroaryl fused tetracyclic indole-based inhibitors of the hepatitis C viral polymerase, NS5B. The introduction of alternative heterocyclic moieties into the indolo-fused inhibitor class significantly expands the reported SAR and resulted in the identification of pyridino analogs, typified by compounds 44 and 45 that displayed excellent potency against the NS5B polymerase of both HCV 1a and HCV 1b genotypes.
Inhibitors of HCV replication
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Page/Page column 181-182, (2010/10/20)
Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.
A FACILE SYNTHESIS OF BROMO-2-ALKOXYPYRIDINES
Shiao, Min-Jen,Tarng, Kai-Yih
, p. 819 - 824 (2007/10/02)
Several bromo-2-methoxypyridines 2a-2e and bromo-2-benzyloxypyridines 2a'-2e' were synthesised by the reaction of bromo-substituted 2-pyridones 1 which were reacted with alkyl halides in the presence of silver carbonate in benzene.
