Design, synthesis and biological evaluation of 2-amino-N-(2-aminophenyl)thiazole-5-carboxamide derivatives as novel Bcr-Abl and histone deacetylase dual inhibitors

Chen Xin; Zhao Shuang; Wu Yichao; Chen Yadong; Lu Tao; Zhu Yong

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Design, synthesis and biological evaluation of 2-amino-N-(2-aminophenyl)thiazole-5-carboxamide derivatives as novel Bcr-Abl and histone deacetylase dual inhibitors

机译：2-氨基-N-（2-氨基苯基）噻唑-5-甲酰胺衍生物作为新型BCR-ABL和组蛋白脱乙酰化酶双抑制剂的设计，合成和生物学评价

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In recent studies, combinations of histone deacetylase (HDAC) inhibitors with kinase inhibitor showed additive and synergistic effects. Herein we present a novel design approach for cancer drug development by combination of breakpoint cluster Abl (Bcr-Abl) and HDAC inhibitory activity, two independent pharmacological activities, in one molecule. The designed compounds were synthesized and tested, showing inhibitory activity against Bcr-Abl and HDAC1. The representative dual Bcr-Abl/ HDAC inhibitors, compounds 6a and 6m, showed potent antiproliferative activities against human leukemia cell line K562 and prostate cancer cell line DU145 in cellular assays. This work may lay the foundation for developing dual Bcr-Abl/HDAC inhibitors as potential anticancer therapeutics.

机译：在最近的研究中，具有激酶抑制剂的组蛋白脱乙酰酶（HDAC）抑制剂的组合显示添加剂和协同作用。在此，我们通过断点聚类ABL（BCR-ABL）和HDAC抑制活性，两个独立的药理学活性，在一个分子中提出了一种新的癌症药物开发的设计方法。合成设计的化合物并测试，显示针对BCR-ABL和HDAC1的抑制活性。代表性的双BCR-ABL / HDAC抑制剂，化合物6a和6m，显示出对人白血病细胞系K562和前列腺癌细胞系DU145的有效的抗增殖活动。这项工作可以为开发双BCR-ABL / HDAC抑制剂作为潜在的抗癌治疗方法奠定基础。

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来源
《RSC Advances》 |2016年第105期|共7页
作者
Chen Xin; Zhao Shuang; Wu Yichao; Chen Yadong; Lu Tao; Zhu Yong;
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China Pharmaceut Univ Sch Sci Dept Organ Chem 639 Longmian Ave Nanjing 211198 Jiangsu Peoples R China;

China Pharmaceut Univ Sch Sci Dept Organ Chem 639 Longmian Ave Nanjing 211198 Jiangsu Peoples R China;

China Pharmaceut Univ Sch Sci Dept Organ Chem 639 Longmian Ave Nanjing 211198 Jiangsu Peoples R China;

China Pharmaceut Univ Sch Sci Lab Mol Design &

Drug Discovery 639 Longmian Ave Nanjing 211198 Jiangsu Peoples R China;

China Pharmaceut Univ Sch Sci Dept Organ Chem 639 Longmian Ave Nanjing 211198 Jiangsu Peoples R China;

China Pharmaceut Univ Sch Sci Dept Organ Chem 639 Longmian Ave Nanjing 211198 Jiangsu Peoples R China;

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正文语种 eng
中图分类化学;
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2. Design, synthesis and biological evaluation of 2-amino-N-(2-aminophenyl)thiazole-5-carboxamide derivatives as novel Bcr-Abl and histone deacetylase dual inhibitors [J] . Chen Xin, Zhao Shuang, Wu Yichao, RSC Advances . 2016,第105期

机译：2-氨基-N-（2-氨基苯基）噻唑-5-甲酰胺衍生物作为新型BCR-ABL和组蛋白脱乙酰化酶双抑制剂的设计，合成和生物学评价
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Design, synthesis and biological evaluation of 2-amino-N-(2-aminophenyl)thiazole-5-carboxamide derivatives as novel Bcr-Abl and histone deacetylase dual inhibitors

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