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1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2005 Jun 30 , DOI: 10.1021/jm050267e Ronghui Lin 1 , Peter J. Connolly 1 , Shenlin Huang 1 , Steven K. Wetter 1 , Yanhua Lu 1 , William V. Murray 1 , Stuart L. Emanuel 1 , Robert H. Gruninger 1 , Angel R. Fuentes-Pesquera 1 , Catherine A. Rugg 1 , Steven A. Middleton 1 , Linda K. Jolliffe 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2005 Jun 30 , DOI: 10.1021/jm050267e Ronghui Lin 1 , Peter J. Connolly 1 , Shenlin Huang 1 , Steven K. Wetter 1 , Yanhua Lu 1 , William V. Murray 1 , Stuart L. Emanuel 1 , Robert H. Gruninger 1 , Angel R. Fuentes-Pesquera 1 , Catherine A. Rugg 1 , Steven A. Middleton 1 , Linda K. Jolliffe 1
Affiliation
A series of 1-acyl-1H-[1,2,4]triazole-3,5-diamine analogues were synthesized as cyclin-dependent kinase (CDK) inhibitors. These compounds showed potent and selective CDK1 and CDK2 inhibitory activities and inhibited in vitro cellular proliferation in various human tumor cells. Representative compound 3b demonstrated in vivo efficacy in a human melanoma A375 xenograft model in nude mice.
中文翻译：
1-酰基-1H- [1,2,4]三唑-3,5-二胺类似物作为新型和有效的抗细胞周期蛋白依赖性激酶抑制剂：合成和生物活性评估。
合成了一系列1-酰基-1H- [1,2,4]三唑-3,5-二胺类似物作为细胞周期蛋白依赖性激酶（CDK）抑制剂。这些化合物显示出有效和选择性的CDK1和CDK2抑制活性，并在各种人类肿瘤细胞中抑制了体外细胞增殖。代表性化合物3b在裸鼠的人黑素瘤A375异种移植模型中证明了体内功效。
更新日期：2017-01-31
中文翻译：
1-酰基-1H- [1,2,4]三唑-3,5-二胺类似物作为新型和有效的抗细胞周期蛋白依赖性激酶抑制剂：合成和生物活性评估。
合成了一系列1-酰基-1H- [1,2,4]三唑-3,5-二胺类似物作为细胞周期蛋白依赖性激酶（CDK）抑制剂。这些化合物显示出有效和选择性的CDK1和CDK2抑制活性，并在各种人类肿瘤细胞中抑制了体外细胞增殖。代表性化合物3b在裸鼠的人黑素瘤A375异种移植模型中证明了体内功效。
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