870543-91-2Relevant academic research and scientific papers
Continuous flow/waste-minimized synthesis of benzoxazoles catalysed by heterogeneous manganese systems
Ferlin, Francesco,Van Der Hulst, Mitchell K.,Santoro, Stefano,Lanari, Daniela,Vaccaro, Luigi
supporting information, p. 5298 - 5305 (2019/10/11)
Herein, we present our results on the development of a waste minimized protocol for the synthesis of 2-arylbenzoxazoles in continuous flow. Manganese-based heterogeneous catalysts were used in combination with cyclopentylmethyl ether as an environmentally friendly and safe reaction medium. The use of oxygen promotes the oxidative process ensuring at the same time a complete regeneration of the catalyst adopting a flow configuration which does not include the use of an additional mechanical pump. These features allowed for a faster synthesis compared to batch procedures with minimal metal leaching.
Phosphorescent host compound and OELD (Organic Electroluminescent Device) thereof
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Paragraph 0055; 0056-0058, (2017/02/24)
The invention provides a phosphorescent host compound, which is as shown in a structural formula I, containing benzothiazole and benzoxazole. The phosphorescent host compound provided by the invention has better thermal stability, high luminous efficiency
Small organic molecules based on oxazole/thiazole with excellent performances in green and red phosphorescent organic light-emitting diodes
Tian, Guojian,Wei, Xiang,Xiang, Ning,Huang, Jinhai,Cao, Jin,Wang, Zixing,Zhang, Jianhua,Su, Jianhua
, p. 51575 - 51582 (2016/06/13)
Four pure organic molecules based on oxazole/thiazole were designed and characterized, and their relevant thermal, photophysical and electrochemical properties were fully investigated. These compounds (2a-2d) exhibited good thermal stabilities, with endot
COMPOUND FOR AN ORGANIC PHOTOELECTRIC DEVICE, ORGANIC PHOTOELECTRIC DEVICE INCLUDING THE SAME, AND DISPLAY DEVICE INCLUDING THE ORGANIC PHOTOELECTRIC DEVICE
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Page/Page column 67, (2013/02/27)
A compound for an organic photoelectric device, an organic photoelectric device including the same, and a display device including the organic photoelectric device, the compound being represented by the following Chemical Formula 1:
COMPOUND FOR ORGANIC PHOTOELECTRIC DEVICE, ORGANIC PHOTOELECTRIC DEVICE INCLUDING THE SAME, AND DISPLAY DEVICE INCLUDING THE SAME
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, (2011/11/06)
A compound for an organic photoelectric device, an organic photoelectric device including the same, and a display device including the same the compound being represented by the following Chemical Formula 1:
Synthesis and pharmacological evaluation of N -(3-(1 H -Indol-4-yl)-5-(2- methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent
Shetty, Rupa S.,Lee, Younghee,Liu, Bin,Husain, Arifa,Joseph, Rhoda W.,Lu, Yixin,Nelson, David,Mihelcic, John,Chao, Wenchun,Moffett, Kristofer K.,Schumacher, Andreas,Flubacher, Dietmar,Stojanovic, Aleksandar,Bukhtiyarova, Marina,Williams, Ken,Lee, Kyoung-Jin,Ochman, Alexander R.,Saporito, Michael S.,Moore, William R.,Flynn, Gary A.,Dorsey, Bruce D.,Springman, Eric B.,Fujimoto, Ted,Kelly, Martha J.
experimental part, p. 179 - 200 (2011/03/19)
The synthesis and optimization of a series of orally bioavailable 1-(1H-indol-4-yl)-3,5-disubstituted benzene analogues as antimitotic agents are described. A functionalized dibromobenzene intermediate was used as a key scaffold, which when modified by sequential Suzuki coupling and Buchwald-Hartwig amination provided a flexible entry to 1,3,5-trisubstituted phenyl compounds. A 1H-indol-4-yl moiety at the 1-position was determined to be a critical feature for optimal potency. The compounds have been shown to induce cell cycle arrest at the G2/M phase and demonstrate efficacy in both cell viability and cell proliferation assays. The primary site of action for these agents is revealed by their colchicine competitive inhibition of tubulin polymerization, and a computational model has been developed for the association of these compounds to tubulin. An optimized lead LP-261 significantly inhibits growth of a human non-small-cell lung tumor (NCI-H522) in a mouse xenograft model.
Anti-cancer agents and uses thereof
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Page/Page column 51, (2008/12/08)
The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.
Biochemical and structural evaluation of highly selective 2-arylbenzoxazole-based transthyretin amyloidogenesis inhibitors
Johnson, Steven M.,Connelly, Stephen,Wilson, Ian A.,Kelly, Jeffery W.
, p. 260 - 270 (2008/09/18)
To develop potent transthyretin (TTR) amyloidogenesis inhibitors that also display high binding selectivity in blood, it proves useful to systematically optimize each of the three substructural elements that comprise a typical inhibitor: the two aryl rings and the linker joining them. In the first study, described herein, structural modifications to one aryl ring were evaluated by screening a library of 2-arylbenzoxazoles bearing thyroid hormone-like aryl substituents on the 2-aryl ring. Several potent and highly selective amyloidogenesis inhibitors were identified that exhibit minimal thyroid hormone nuclear receptor and COX-1 binding. High resolution crystal structures (1.3-1.5 ?) of three inhibitors (2f, 4f, and 4d) in complex with TTR were obtained to characterize their binding orientation. Collectively, the results demonstrate that thyroid hormone-like substitution patterns on one aryl ring lead to potent and highly selective TTR amyloidogenesis inhibitors that lack undesirable thyroid hormone receptor or COX-1 binding.
