Dinuclear ruthenium(II)-NNN complexes were efficiently assembled by means of coordinatively unsaturated 16-electron mononuclear ruthenium(II)-pyrazolyl-imidazolyl-pyridine complex and 4,4′-linked bipyridine ligands. The diruthenium(II)-NNN complex assembledthrough 4,4′-(CH2)3-bipyridine exhibited exceptionally high catalytic activity for the transfer hydrogenation (TH) of ketones in refluxing 2-propanol
借助配位不饱和的16电子单核钌(II)-吡唑基-咪唑基-吡啶配合物和4,4'-连接的联吡啶配体有效地组装了双核钌(II)-NNN配合物。通过4,4'-(CH 2)3-联吡啶组装的二钌(II)-NNN络合物在回流的2-丙醇中对酮的转移加氢(TH)表现出极高的催化活性,并且TOF值高达1.4×10 7 h – 1,表明钌(II)-NNN功能具有显着的协同作用。
BENZIMIDAZOLE DERIVATIVES AS BROMODOMAIN INHIBITORS
申请人:Gilead Sciences, Inc.
公开号:US20140336190A1
公开(公告)日:2014-11-13
This application relates to chemical compounds which may act as inhibitors of; or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I)
wherein R
1a
, R
1b
, R
2
, R
2b
, R
3
, R
4a
, R
4b
, and R
5
are described herein.
The invention relates to a compound of the formula
wherein the substituents are as defined herein, and a pharmaceutically acceptable salt of the compound of formula (1). The compounds of formula (1) and their salts possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations such as inflammatory joint diseases. The compounds of formula (1) are also useful for the treatment of diseases where chronic inflammation is the underlying cause. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds, and their use for the preparation of a medicament for the treatment of humans and animals.
The invention relates to a compound of the formula
wherein the substituents are as defined herein, and a pharmaceutically acceptable salt of the compound of formula (1). The compounds of formula (1) and their salts possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations such as inflammatory joint diseases. The compounds of formula (1) are also useful for the treatment of diseases where chronic inflammation is the underlying cause. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds, and their use for the preparation of a medicament for the treatment of humans and animals.
Aerobic Oxidation of in Situ Generated Cyanine Dyes Leading to DNA Damage
作者:Anastasiia A. Tikhomirova、Nikolai A. Tcyrulnikov、R. Marshall Wilson
DOI:10.1021/acs.orglett.9b00194
日期:2019.3.1
oxidation of pyridinocyanine dyes is described. The dyes are generated in situ during spontaneous oxidations of tetrakis- and bis(N-methylpyridin-4-ium)alkane salts. The mechanism of aerobic oxidation of the latter compound is proposed, and a rare direct catalyst-free transition from saturated alkane to a gem-diol is demonstrated. Thermal DNA oxidation by cyaninedyes has potential in ROS-based cancer