383868-64-2Relevant articles and documents
WDR5-MYC INHIBITORS
-
Paragraph 00516; 00804; 00806; 001471-001472, (2021/02/05)
Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
Decreasing HepG2 Cytotoxicity by Lowering the Lipophilicity of Benzo[d]oxazolephosphinate Ester Utrophin Modulators
Chatzopoulou, Maria,Emer, Enrico,Lecci, Cristina,Rowley, Jessica A.,Casagrande, Anne-Sophie,Moir, Lee,Squire, Sarah E.,Davies, Stephen G.,Harriman, Shawn,Wynne, Graham M.,Wilson, Francis X.,Davies, Kay E.,Russell, Angela J.
supporting information, p. 2421 - 2427 (2020/12/03)
Utrophin modulation is a disease-modifying therapeutic strategy for Duchenne muscular dystrophy that would be applicable to all patient populations. To improve the suboptimal profile of ezutromid, the first-in-class clinical candidate, a second generation
Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction
Macdonald, Jonathan D.,Chacón Simon, Selena,Han, Changho,Wang, Feng,Shaw, J. Grace,Howes, Jennifer E.,Sai, Jiqing,Yuh, Joannes P.,Camper, Demarco,Alicie, Bethany M.,Alvarado, Joseph,Nikhar, Sameer,Payne, William,Aho, Erin R.,Bauer, Joshua A.,Zhao, Bin,Phan, Jason,Thomas, Lance R.,Rossanese, Olivia W.,Tansey, William P.,Waterson, Alex G.,Stauffer, Shaun R.,Fesik, Stephen W.
, p. 11232 - 11259 (2019/12/25)
The treatment of tumors driven by overexpression or amplification of MYC oncogenes remains a significant challenge in drug discovery. Here, we present a new strategy toward the inhibition of MYC via the disruption of the protein-protein interaction betwee
IDO INHIBITORS
-
Page/Page column 101; 102, (2015/01/16)
There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
A practical nickel-catalyzed reductive alkylation of amidophenyl bromides
Liu, Xuge,Yang, Zhilin,Li, Ya-Min,Yang, Fan,Feng, Liang,Wang, Nengzhong,Ma, Debiao,Chang, Kwen-Jen,Shen, Yuehai
, p. 9522 - 9529 (2015/03/04)
A modified Weix's reductive coupling for alkylation of amidoaryl bromides based on Ni(COD)2 precatalyst and 2,2′-dipyridyl ligand was developed. This reaction is reliable for amidophenyl bromides and gives yields up to 87%, and is potentially useful in the synthesis of amidophenyl-containing molecules.
INHIBITORS OF SPHINGOSINE KINASE 1
-
Page/Page column 98, (2010/04/25)
The invention relates to compounds of Formula (I). Compounds of the present invention are inliibitors of sphingosine kinase 3, and are useful in the treatment of various disorders and conditions, such as inflammatory disorders
Boron-containing phenoxyacetanilide derivatives as hypoxia-inducible factor (HIF)-1α inhibitors
Shimizu, Kazuki,Maruyama, Minako,Yasui, Yuka,Minegishi, Hidemitsu,Ban, Hyun Seung,Nakamura, Hiroyuki
scheme or table, p. 1453 - 1456 (2010/07/06)
A series of boron-containing phenoxyacetanilide derivatives 8a-f, 9a-f, 15, and 16 were synthesized as hypoxia-inducible factor (HIF)-1α inhibitors. Among the compounds synthesized, carboranylphenoxyacetanilide 16 (GN26361) was found to be a potent inhibitor against HIF-1α accumulation under hypoxic conditions and inhibited the hypoxia-induced HIF-1 transcriptional activity in HeLa cells (IC50 = 0.74 μM). Compound 16 suppressed hypoxia-induced HIF-1α accumulation and vascular endothelial growth factor mRNA expression in a concentration-dependent manner without affecting the expression of HIF-1α mRNA.
PHENYLALANINE AMIDE DERIVATIVES USEFUL FOR TREATING INSULIN-RELATED DISEASES AND CONDITIONS
-
Page/Page column 60, (2010/09/03)
Provided herein are compounds of formula I: wherein A, B, X, R1 , R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions
Synthesis and in-vitro biological activity of macrocyclic urea Chk1 inhibitors
Li, Gaoquan,Tao, Zhi-Fu,Tong, Yunsong,Przytulinska, Magdalena K.,Kovar, Peter,Merta, Philip,Chen, Zehan,Zhang, Haiying,Sowin, Thomas,Rosenberg, Saul H.,Lin, Nan-Horng
, p. 6499 - 6504 (2008/03/18)
A variety of macrocyclic urea compounds were prepared as potent Chk1 inhibitors by modifying the C5 position of the benzene ring of the macrocyclic urea with ether moieties, aliphatic carbon chains, amide and halides. Enzymatic activity less than 20 nM was observed in 29 of 40 compounds. Compounds 14, 46d, and 48j provided the best overall results in the cellular assays as they abrogated doxorubicin-induced cell cycle arrest (IC50 = 3.31, 3.08, and 3.13 μM) and enhanced doxorubicin cytotoxicity (IC50 = 0.54, 1.27, and 0.96 μM) while displaying no single agent activity, respectively.
l , l , 3-TRI0X0-l , 2 , 5-THIADIAZ0LIDINES AND THEIR USE AS PTP-ASES INHIBITORS
-
Page/Page column 38, (2010/11/27)
Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other e