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Synthesis of novel pyrazole carboxamide derivatives and discovery of modulators for apoptosis or autophagy in A549 lung cancer cells
被引:47
|作者:
Ding, Xiao-Ling
[1
,3
]
Zhang, Hai-Yan
[2
]
Qi, Lei
[2
]
Zhao, Bao-Xiang
[1
]
Lian, Song
[1
]
Lv, Hong-Shui
[1
]
Miao, Jun-Ying
[2
]
机构:
[1] Shandong Univ, Sch Chem & Chem Engn, Inst Organ Chem, Jinan 250100, Peoples R China
[2] Shandong Univ, Sch Life Sci, Inst Dev Biol, Jinan 250100, Peoples R China
[3] Qingdao Univ, Coll Adv Profess Technol, Qingdao 266061, Peoples R China
基金:
中国国家自然科学基金;
关键词:
Pyrazole;
Carboxamide;
A549;
cells;
Apoptosis;
Autophagy;
BIOLOGICAL EVALUATION;
RECEPTOR ANTAGONISTS;
POTENTIAL AGENTS;
DESIGN;
INHIBITORS;
D O I:
10.1016/j.bmcl.2009.07.131
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
A series of novel 3-aryl-1-arylmethyl-1H-pyrazole-5-carboxamide derivatives 3a-1, were synthesized by the reaction of 3-aryl-1-arylmethyl-1H-pyrazole-5-carbonyl chloride with substituted amine in excellent yields. The compounds 3e-h could suppress A549 lung cancer cell growth, More interestingly, compounds 3e and 3f might inhibit the A549 cell growth by inducing apoptosis; whereas compounds 3g and 3h with fluorine group might inhibit the A549 cell growth by inducing autophagy. (C) 2009 Elsevier Ltd. All rights reserved.
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页码:5325 / 5328
页数:4
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