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Synthesis and Biological Evaluation of Novel 4-(4-Formamidophenylamino)-N-methylpicolinamide Derivatives as Potential Antitumor Agents.

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机构: [1]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University and Collaborative Innovation Center, Chengdu 610041, China [2]Hairong Research Institute, Sichuan Hairong Pharmaceutical Co., Ltd., Yangtze River Pharmaceutical Group, Chengdu 611830, China [3]Open Laboratory, West China Institute of Women and Children’s Health, West China Second University Hospital, Sichuan University, Chengdu 610041, China
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关键词: 4-(4-formamidophenylamino)-N-methylpicolinamide derivatives anti-proliferation angiogenesis inhibitors apoptosis pharmacology

摘要:
A novel series of 4-(4-formamidophenylamino)-N-methylpicolinamide derivatives were synthesized and evaluated against different tumor cell lines. Experiments in vitro showed that these derivatives could inhibit the proliferation of two kinds of human cancer cell lines (HepG2, HCT116) at low micromolar concentrations and the most potent analog 5q possessed broad-spectrum antiproliferative activity. Experiments in vivo demonstrated that 5q could effectively prolong the longevity of colon carcinoma-burdened mice and slow down the progression of cancer cells by suppression of angiogenesis and the induction of apoptosis and necrosis.

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出版当年[2021]版:
大类 | 3 区 化学
小类 | 3 区 生化与分子生物学 3 区 化学综合
最新[2023]版:
大类 | 2 区 化学
小类 | 3 区 生化与分子生物学 3 区 化学:综合
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第一作者机构: [1]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University and Collaborative Innovation Center, Chengdu 610041, China [2]Hairong Research Institute, Sichuan Hairong Pharmaceutical Co., Ltd., Yangtze River Pharmaceutical Group, Chengdu 611830, China
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