- Novel 2, 8-bit derivatives of quinolines attenuate Pseudomonas aeruginosa virulence and biofilm formation
-
Signal molecules are stimulators of multiple quroum-sensing virulence and biofilm formation. Small molecule analogues have been suspected as a potent inhibitor in therapeutic strategy. Herein, we synthesized a series of small molecule compounds from the 2
- Qiu, Man-Na,Wang, Fang,Chen, Si-Yu,Wang, Peng-Cheng,Fu, Yu-Hang,Liu, Yuan-Yuan,Wang, Xuan,Wang, Fan-Bei,Wang, Chao,Yang, Hong-Wen,Wu, Yang,Zhu, Shi-Ying,Zhou, Hai-Bo,Chen, Wei-Min,Lin, Jing,Zheng, Jun-Xia,Sun, Ping-Hua
-
-
Read Online
- Structure-activity relationships of anticancer ruthenium(II) complexes with substituted hydroxyquinolines
-
8-Hydroxyquinolines (HQ), including clioquinol, possess cytotoxic properties and are widely used as ligands for metal-based anticancer drug research. The number and identity of substituents on the HQ can have a profound effect on activity for a variety of inorganic compounds. Ruthenium complexes of HQ exhibit radically improved potencies, and operate by a new, currently unknown, mechanism of action. To define structure-activity relationships (SAR), a family of 22 Ru(II) coordination complexes containing mono-, di- and tri-substituted hydroxyquinoline ligands were synthesized and their biological activity evaluated. The complexes exhibited promising cytotoxic activity against a cancer cell line, and the SAR data revealed the 2- and 7-positions as key sites for the incorporation of halogens to improve potency. The Ru(II) complexes potently inhibited translation, as demonstrated by an in-cell translation assay. The effects were seen at 2–15-fold higher concentrations than those required to observe cytotoxicity, suggesting that prevention of protein synthesis may be a primary, but not the exclusive mechanism for the observed cytotoxic activity.
- Havrylyuk, Dmytro,Howerton, Brock S.,Nease, Leona,Parkin, Sean,Heidary, David K.,Glazer, Edith C.
-
-
Read Online
- Organic optoelectronic functional material and application thereof
-
The invention belongs to the field of organic electroluminescent devices, and discloses an organic electroluminescent material containing a diquinolyl structure and application of the organic electroluminescent material. By using the organic electroluminescent material provided by the invention as an electron transport material, the produced device has good electron mobility and relatively-balanced current carrier transmission property, and the improvement efficiency of the device is facilitated. In addition, the organic electroluminescent material provided by the invention also can be furtherblended with a hole type main body material so as to form an exciplex; by using the exciplex as a co-subject material, the efficiency and the stability of the produced device are both improved obviously.
- -
-
-
- Heteroaryl cross-coupling as an entry toward the synthesis of lavendamycin analogues: A model study
-
(Chemical Equation Presented) ABC analogues of the antitumor antibiotic lavendamycin, which contain the key metal chelation site and redox-active quinone unit essential for biological activity, were prepared via the palladium(0)-catalyzed cross-coupling reaction of various 2-haloheteroaromatics with 2-stannylated pyridines and quinolines. Using the Stille reaction, 2-bromo substituted quinolines and 1-bromoisoquinolines were found to undergo efficient coupling with 2-pyridinylstannanes to provide unsymmetrical heterobiaryl derivatives. While the Stille reaction using the reverse coupling partners (i.e., 2-quinolinylstannanes and haloheteroaromatics) had not received much attention in the literature, we found that this alternative coupling reaction efficiently provided several new heterobiaryl derivatives. The gold-catalyzed intramolecular cycloisomerization of N-(prop-2-ynyl)-1H-indole-2-carboxamide smoothly afforded a β-carbolinone derivative that was subsequently used for a Pd(0)-catalyzed cross-coupling directed toward the synthesis of lavendamycin analogues.
- Verniest, Guido,Wang, Xingpo,De Kimpe, Norbert,Padwa, Albert
-
experimental part
p. 424 - 433
(2010/03/30)
-
- Improved Syntheses of Some Monohloro- and Monobromo-8-quinolinols
-
Procedures were developed for the preparation of the 2-, 3-, 4-, and 6-monosubstituted chloro and bromo 8-quinolinols which afforded greater yields and/or reduced the number of steps in the preparation. 100 MHz 1H-NMR spetra for the 12 possible monochloro
- Gershon, Herman,Clarke, Donald D.
-
p. 935 - 942
(2007/10/02)
-