74864-94-1Relevant academic research and scientific papers
ORGANIC ELECTROLUMINESCENT COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME
-
Paragraph 0158-0159; 0162-0163, (2020/05/01)
The present application relates to an organic electroluminescent compound represented by chemical formula 1, and an organic electroluminescent device comprising the same. By comprising the organic electroluminescent compound of the present application having good thermal stability, it is possible to provide the organic electroluminescent device having lower driving voltage, high luminous efficiency and/or long lifespan characteristics compared with an existing organic electroluminescent device.COPYRIGHT KIPO 2020
Design, synthesis and biological evaluation of novel 4-phenoxypyridine based 3-oxo-3,4-dihydroquinoxaline-2-carboxamide derivatives as potential c-Met kinase inhibitors
Wang, Zhen,Shi, Jiantao,Zhu, Xianglong,Zhao, Wenwen,Gong, Yilin,Hao, Xuechen,Hou, Yunlei,Liu, Yajing,Ding, Shi,Liu, Ju,Chen, Ye
, (2020/10/21)
Blocking c-Met kinase activity by small-molecule inhibitors has been identified as a promising approach for the treatment of cancers. Herein, we described the design, synthesis, and biological evaluation of a series of 4-phenoxypyridine-based 3-oxo-3,4-dihydroquinoxaline derivatives as c-Met kinase inhibitors. Inhibitory activitives against c-Met kinase evaluation indicated that most of compounds showed excellent c-Met kinase activity in vitro, and IC50 values of ten compounds (23a, 23e, 23f, 23l, 23r, 23s, 23v, 23w, 23x and 23y) were less than 10.00 nM. Notably, three of them (23v, 23w and 23y) showed remarkable potency with IC50 values of 2.31 nM, 1.91 nM and 2.44 nM, respectively, and thus they were more potent than positive control drug foretinib (c-Met, IC50 = 2.53 nM). Cytotoxic evaluation indicated the most promising compound 23w showed remarkable cytotoxicity against A549, H460 and HT-29 cell lines with IC50 values of 1.57 μM, 0.94 μM and 0.65 μM, respectively. Furthermore, the acridine orange/ethidium bromide (AO/EB) staining, cell apoptosis assays by flow cytometry, wound-healing assays and transwell migration assays on HT-29 and/or A549 cells of 23w were performed. Especially compound 23w, which displayed potent antitumor, apoptosis induction and antimetastatic activity, could be used as a promising lead for further development. Meanwhile, their preliminary structure-activity relationships (SARs) were also discussed.
Design, synthesis and biological evaluation of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydroquinoxaline moiety as c-Met kinase inhibitors
Liu, Ju,Yang, Di,Yang, Xiuxiu,Nie, Minhua,Wu, Guodong,Wang, Zhunchao,Li, Wei,Liu, Yajing,Gong, Ping
, p. 4475 - 4486 (2017/07/22)
A series of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydroquinoxaline moiety were synthesized and evaluated for their c-Met kinase inhibitory activity and antiproliferative activity against five cancer cell lines (HT-29, H460, A549, MKN-45 and U87MG) in vitro. Most of the compounds exhibited moderate-to-significant cytotoxicity as compared with foretinib. The most promising compound 41 (with c-Met IC50 value of 0.90?nM) showed remarkable cytotoxicity against HT-29, H460, A549, MKN-45 and U87MG cell lines with IC50 values of 0.06?μM, 0.05?μM, 0.18?μM, 0.023?μM and 0.66?μM, respectively, and thus it was 1.22- to 3.50-fold more potent than foretinib. Their preliminary structure-activity relationships (SARs) studies indicate that electron-withdrawing groups on the terminal phenyl rings are beneficial for improving the antitumor activity.
MULTICYCLIC COMPOUND INCLUDING NITROGEN AND ORGANIC LIGHT EMITTING DEVICE USING THE SAME
-
Paragraph 0120; 0121; 0124; 0125, (2016/10/10)
The present invention relates to a polycyclic compound containing nitrogen, and an organic light emitting device comprising the same. The organic light emitting device of the present invention comprises a positive electrode, a negative electrode, and one
Palladium-catalyzed domino double n-arylations (inter- and intramolecular) of 1,2-diamino(hetero)arenes with o,o-dihalo(hetero)arenes for the synthesis of phenazines and pyridoquinoxalines
Laha, Joydev K.,Tummalapalli, K.S. Satyanarayana,Gupta, Ankur
, p. 8330 - 8335 (2014/01/06)
Domino reactions for the synthesis of phenazines have been developed that start from 1,2-diaminoarenes and 1,2-dihaloarenes and proceed through palladium-catalyzed double N-arylations (inter- and intramolecular) followed by an in situ oxidation. A variety of functional groups, which include base-sensitive groups, were well tolerated under the optimized reaction conditions to afford phenazines in good to excellent yields. The protocol was extended to the synthesis of pyridoquinoxalines by employing either o-phenylenediamines and 2,3-dihalopyridines or 1,2-diaminopyridines and 1,2-dihaloarenes. Domino reactions for the synthesis of phenazines have been developed that start from 1,2-diaminoarenes and 1,2-dihaloarenes and proceed through palladium-catalyzed double N-arylations (inter- and intramolecular) followed by an in situ oxidation. The protocol was extended to the synthesis of pyridoquinoxalines. Copyright
Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-Aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3 H)-yl]-1-(methylamino)butan-2- ols (WYE-103231)
O'Neill, David J.,Adedoyin, Adedayo,Alfinito, Peter D.,Bray, Jenifer A.,Cosmi, Scott,Deecher, Darlene C.,Fensome, Andrew,Harrison, Jim,Leventhal, Liza,Mann, Charles,McComas, Casey C.,Sullivan, Nicole R.,Spangler, Taylor B.,Uveges, Albert J.,Trybulski, Eugene J.,Whiteside, Garth T.,Zhang, Puwen
experimental part, p. 4511 - 4521 (2010/08/20)
Structural modification of a virtual screening hit led to the identification of a new series of 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol- 1(3H)-yl]-1-(methylamino)butan-2-ols which are potent and selective inhibitors of the norepinephrine transporter over both the serotonin and dopamine transporters. One representative compound S-17b (WYE-103231) had low nanomolar hNET potency (IC50 = 1.2 nM) and excellent selectivity for hNET over hSERT (>1600-fold) and hDAT (>600-fold). S-17b additionally had a good pharmacokinetic profile and demonstrated oral efficacy in rat models of ovariectomized-induced thermoregulatory dysfunction and morphine dependent flush as well as the hot plate and spinal nerve ligation (SNL) models of acute and neuropathic pain.
ARYL SULFAMIDE DERIVATIVES AND METHODS OF THEIR USE
-
Page/Page column 143, (2008/12/06)
The present invention is directed to aryl sulfamide derivatives of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
Electrochemical Reactions. Part 24. Reductive Cyclisation of i-(2-Halogenophenyl)-j-phenyl Compounds: A General Reaction
Grimshaw, James,Hamilton, Robert,Trocha-Grimshaw, Jadwiga
, p. 229 - 234 (2007/10/02)
The phenyl ?-radical formed by reduction of aryl halides in an aprotic solvent undergoes efficient radical substitution on an adjacent benzene ring.Several examples of this cyclisation reaction are given.The reaction is appropriate for the synthesis of 6-membered aromatic rings where the two reacting phenyl groups are held in a cis-configuration by an olefin bond or another aromatic ring.
