17071-24-8Relevant academic research and scientific papers
Tariquidar-Related Chalcones and Ketones as ABCG2 Modulators
Pe?a-Solórzano, Diana,Scholler, Matthias,Bernhardt, Günther,Buschauer, Armin,K?nig, Burkhard,Ochoa-Puentes, Cristian
, p. 854 - 859 (2018)
ABC transporters, including ABCG2, play a vital role in defending the human body against the vast range of xenobiotics. Even though this is beneficial for human health, these protein transporters have been implicated in the emerging resistance of cancer c
A biomimetic approach towards phorone sesterterpenoids
Shirley, Harry J.,Bray, Christopher D.
, p. 6985 - 6988 (2019)
We report an investigation towards a unified total synthesis of the Korean sponge derived sesterterpenoids, phorones A (1) and B (2), via a biomimetic strategy. This work has established a new synthetic strategy to the parent ansellane sesterterpenoid ske
THIAZOLIDINONE COMPOUNDS AND USE THEREOF
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Paragraph 0243-0244, (2017/09/21)
A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.
Dihydrothiazolone compounds containing sulfamide and pharmaceutical compositions and use thereof
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Paragraph 0130; 0131; 0132; 0133, (2016/10/08)
The invention provides dihydrothiazolone compounds containing sulfamide, represented by a formula (I), pharmaceutical compositions and use thereof. The compounds can be combined with proteins with bromodomain structural domains so as to adjust a downstream signal channel and exert a special function, and can be used for treating many diseases associated with bromodomain structural domains. The compounds can interfere combination of Brd4 with the bromodomain structural domain and an acetylized histone so as to down-regulate transcription of a cancer gene c-myc and associated target genes thereof, so that the compounds can become effective therapeutic drugs for treating tumors.
Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors
Murray, Christopher W.,Berdini, Valerio,Buck, Ildiko M.,Carr, Maria E.,Cleasby, Anne,Coyle, Joseph E.,Curry, Jayne E.,Day, James E. H.,Day, Phillip J.,Hearn, Keisha,Iqbal, Aman,Lee, Lydia Y. W.,Martins, Vanessa,Mortenson, Paul N.,Munck, Joanne M.,Page, Lee W.,Patel, Sahil,Roomans, Susan,Smith, Kirsten,Tamanini, Emiliano,Saxty, Gordon
supporting information, p. 798 - 803 (2015/07/15)
The DDR1 and DDR2 receptor tyrosine kinases are activated by extracellular collagen and have been implicated in a number of human diseases including cancer. We performed a fragment-based screen against DDR1 and identified fragments that bound either at th
Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization
Zhao, Lele,Wang, Yingqing,Cao, Danyan,Chen, Tiantian,Wang, Qi,Li, Yanlian,Xu, Yechun,Zhang, Naixia,Wang, Xin,Chen, Danqi,Chen, Lin,Chen, Yue-Lei,Xia, Guangxin,Shi, Zhe,Liu, Yu-Chih,Lin, Yijyun,Miao, Zehong,Shen, Jingkang,Xiong, Bing
, p. 1281 - 1297 (2015/03/04)
The signal transduction of acetylated histone can be processed through a recognition module, bromodomain. Several inhibitors targeting BRD4, one of the bromodomain members, are in clinical trials as anticancer drugs. Hereby, we report our efforts on discovery and optimization of a new series of 2-thiazolidinones as BRD4 inhibitors along our previous study. In this work, guided by crystal structure analysis, we reversed the sulfonamide group and identified a new binding mode. A structure-activity relationship study on this new series led to several potent BRD4 inhibitors with IC50 of about 0.05-0.1 μM in FP binding assay and GI50 of 0.1-0.3 μM in cell based assays. To complete the lead-like assessment of this series, we further checked its effects on BRD4 downstream protein c-Myc, investigated its selectivity among five different bromodomain proteins, as well as the metabolic stability test, and reinforced the utility of 2-thiazolidinone scaffold as BET bromodomain inhibitors in novel anticancer drug development.
IMIDAZO-CONDENSED BICYCLES AS INHIBITORS OF DISCOIDIN DOMAIN RECEPTORS (DDRS)
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Page/Page column 86; 87, (2015/02/02)
The invention provides a compound of formula (I) (Formula (I)) or a tautomeric form, stereochemically isomeric form, N-oxide, pharmaceutically acceptable salt or solvate thereof, wherein R2, R3, R4, Ra, Rb
Synthesis, insecticidal activities and SAR of novel phthalamides targeting calcium channel
Chen, Youwei,Li, Yuxin,Pan, Li,Liu, Jingbo,Wan, Yingying,Chen, Wei,Xiong, Lixia,Yang, Na,Song, Haibin,Li, Zhengming
, p. 6366 - 6379 (2015/01/09)
In order to find novel and environmental friendly insecticides targeting the ryanodine receptor, three series of novel phthalamides containing heptafluoroisopropyl group, low fluorine atoms group and non-fluorine group were designed and synthesized. 35 novel structures of three series were obtained. Insecticidal activities of title compounds against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella) indicated that most of title compounds showed moderate to high activities at the tested concentration. The structure-activity relationship (SAR) was discussed in detail. During synthesizing title compounds B8, C7, D1, D9 and D12, their corresponding positional isomers (B8′, C7′, D1′, D9′ and D12′) were afforded, and their structures were confirmed by 2D NMR. The calcium-imaging technique was also applied to investigate the effects of compounds B2, B10, C4 and C5 on the intracellular calcium ion concentration ([Ca2+]i), which indicated that they released stored calcium ions from endoplasmic reticulum, which denoted that some compounds are potential modulators of the insect ryanodine receptor (RyR).
Palladium-catalyzed oxidative acetoxylation of benzylic C-H bond using bidentate auxiliary
Ju, Long,Yao, Jinzhong,Wu, Zaihong,Liu, Zhanxiang,Zhang, Yuhong
, p. 10821 - 10831 (2013/11/19)
Pd(OAc)2-catalyzed oxidative acetoxylation of benzylic C-H bonds utilizing a bidentate system has been explored. A variety of picolinoyl- or quinoline-2-carbonyl-protected toluidine derivatives react with PhI(OAc) 2 in the presence of Pd(OAc)2 to afford the acetoxylated products in synthetically useful yields. A broad of functionalities, such as CH3, F, Cl, Br, I, COCH3, CO2Et, SO 2CH3, and NO2, were tolerated. This transformation provides easy access to 2-hydroxymethylaniline derivatives.
3-BENZYLOXYPHENYLOXOACETIC ACID COMPOUNDS FOR REDUCING URIC ACID
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Page/Page column 26, (2012/10/07)
Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I) or its pharmaceutically acceptable salts. The uric acid-lowering effects of the compounds of this invention are used to treat or
