- Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity
-
Receptor tyrosine kinase PDGFRα is often constitutively activated in various tumours and is regarded as a drug target. Here, we present a collection of 2,6,9-trisubstituted purines with nanomolar potency against PDGFRα and strong and selective cytotoxicity in the human eosinophilic leukaemia cell line EOL-1 that expresses the FIP1L1-PDGFRA oncogene. In treated EOL-1 cells, the example compound 14q inhibited the autophosphorylation of PDGFRα and the phosphorylation of STAT3 and ERK1/2. Interestingly, we observed pronounced and even increased effects of 14q on PDGFRα and some of its downstream signalling pathways after drug washout. In accordance with suppressed PDGFRα signalling, treated cells were arrested in the G1 phase of the cell cycle and eventually underwent apoptosis. Our results show that substituted purines can be used as specific modulators of eosinophilic leukaemia.
- ?ezní?ková, Eva,Gucky, Tomá?,Ková?ová, Veronika,Ajani, Haresh,Jorda, Radek,Kry?tof, Vladimír
-
-
- An active catalytic system for Suzuki-Miyaura cross-coupling reactions using low levels of palladium loading
-
An easily available Pd(OAc)2/(2-(anthracen-9-yl)-1H-inden-3-yl) dicyclohexylphosphine/toluene/iPrOH/water catalytic system was developed, which shows high catalytic activity in the Suzuki-Miyaura cross-coupling reactions of a diverse array of aryl and heteroaryl chlorides with Pd loadings down to 0.01 mol%.
- Yan, Meng-Qi,Yuan, Jia,Lan, Fang,Zeng, Si-Hao,Gao, Meng-Yue,Liu, Sheng-Hua,Chen, Jian,Yu, Guang-Ao
-
supporting information
p. 3924 - 3929
(2017/07/10)
-
- Cross-coupling study of iodo/chloropyridines and 2-chloroquinoline with atom-economic triarylbismuth reagents under Pd-catalysis
-
This study describes the palladium-catalyzed couplings of iodopyridines, chloropyridines, and chloroquinoline with atom-economic BiAr3 reagents in sub-stoichiometric loadings. Mono-arylations of iodo and chloropyridines produced arylpyridines i
- Rao, Maddali L.N.,Dhanorkar, Ritesh J.
-
p. 338 - 349
(2015/03/04)
-
- Palladium(II) catalyzed Suzuki/Sonogashira cross-coupling reactions of sulfonates: An efficient approach to C2-functionalized pyrimidines and pyridines
-
Pyrimidin-2-yl sulfonates, as a reaction partner, can be easily prepared from inexpensive commercial materials and are efficiently cross-coupled with arylboronic acids and terminal alkynes by using Pd(OAc)2-catalyzed Suzuki and Sonogashira reactions. A wide array of C2-functionalized pyrimidines have been prepared in good to excellent yields. 2-Arylpyridines and 2-(oct-1-ynyl)pyridine were also synthesized. An efficient means to synthesize expanded pyrimidin-2-yl conjugated systems was developed by using Pd(OAc) 2-catalyzed cross-coupling reaction of pyrimidin/pyridin-2-yl sulfonates with arylboronic acids and terminal alkynes. Compared with 2-chloropyrimidines, pyrimidin-2-yl sulfonates can be easily prepared from inexpensive commercial materials and the reactions are more efficient. Copyright
- Quan, Zheng-Jun,Jing, Fu-Qiang,Zhang, Zhang,Da, Yu-Xia,Wang, Xi-Cun
-
supporting information
p. 7175 - 7183
(2013/11/06)
-
- NAPHTHALENE DERIVATIVE
-
The present invention provides compounds which can regulate VCP activity. The present invention provides the compound of formula (I) (R is as defined in the description) or oxides, esters, prodrugs, pharmaceutically acceptable salts or solvates thereof. The compounds can regulate VCP activity, and thus are useful for treating VCP-mediated diseases such as neurodegenerative diseases.
- -
-
Paragraph 0255
(2013/06/27)
-
- AGENT FOR TREATMENT OF EYE DISEASES
-
The present invention provides agents effective to treat eye diseases, pharmaceutical compositions comprising them, methods for preparing pharmaceuticals for treatment of eye diseases comprising using the agents, use of the agents in manufacture of pharma
- -
-
Paragraph 0079-0080; 0139-0140
(2013/08/15)
-
- A highly active catalytic system for Suzuki-Miyaura cross-coupling reactions of aryl and heteroaryl chlorides in water
-
An easily available Pd(OAc)2/(2-mesitylindenyl) dicyclohexylphosphine/Me(octyl)3N+Cl-/K 3PO4·3H2O catalytic system was developed and it shows high catalytic activity in the Suzuki-Miyaura cross-coupling reaction of a diverse array of aryl and heteroaryl chlorides in water. Notably, this catalytic system also works with ultra-low loading of the catalyst with high turnover numbers.
- Mao, Shu-Lan,Sun, Yue,Yu, Guang-Ao,Zhao, Cui,Han, Zhi-Jun,Yuan, Jia,Zhu, Xiaolei,Yang, Qihua,Liu, Sheng-Hua
-
p. 9410 - 9417
(2013/01/15)
-
