Ligand-free Pd-catalyzed C-N cross-coupling/cyclization strategy: An unprecedented access to 1-thienyl pyrroloquinoxalines for the new approach towards apoptosis

被引:8
|
作者
Kolli, Sunder Kumar [1 ]
Nakhi, Ali [2 ]
Archana, Sivakumar [2 ,3 ]
Saridena, Maneesha [2 ]
Deora, Girdhar Singh [4 ]
Yellanki, Swapna [2 ,5 ]
Medisetti, Raghavender [2 ,5 ]
Kulkarni, Pushkar [2 ,5 ]
Raju, R. Ramesh [1 ]
Pal, Manojit [2 ]
机构
[1] Acharya Nagarjuna Univ, Dept Chem, Guntur 522510, AP, India
[2] Dr Reddys Inst Life Sci, Hyderabad 500046, Andhra Pradesh, India
[3] Manipal Univ, Manipal Coll Pharmaceut Sci, Manipal 576104, Karnataka, India
[4] Univ Queensland, Sch Pharm, Brisbane, Qld 4072, Australia
[5] Zephase Therapeut, Hyderabad 500046, Andhra Pradesh, India
关键词
Palladium; Pyrroloquinoxaline; PDE4; Apoptosis; Zebrafish; CRYSTAL-STRUCTURE ANALYSIS; ANTICANCER AGENTS; INHIBITORS; DERIVATIVES; THIOPHENE; DESIGN; CELLS; ASSAY;
D O I
10.1016/j.ejmech.2014.08.057
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The link between PDE4 and apoptosis prompted us to design and synthesize for the first time a series of novel 1-thienyl pyrroloquinoxalines as potential PDE4 inhibitors/apoptotic agents. A ligand-free Pd-catalyzed C-N cross-coupling/cyclization strategy has been developed for the rapid and milder access to this class of compounds some of which showed interesting pharmacological properties when tested in vitro and in zebrafish embryos. (C) 2014 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:270 / 278
页数:9
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