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

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

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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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《RSC Advances》 |2016年第105期|共7页
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Xin Chen; Shuang Zhao; Yichao Wu; Yadong Chen; Tao Lu; Yong Zhu;
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1. 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
2. Design, Synthesis and Biological Evaluation of Novel Benzoylimidazole Derivatives as Raf and Histone Deacetylases Dual Inhibitors [J] . Xin Chen, Guoliang Gong, Xinyang Chen, Chemical and Pharmaceutical Bulletin . 2019,第10期

机译：新型苯并咪唑衍生物作为Raf和组蛋白脱乙酰基酶双重抑制剂的设计，合成和生物学评价
3. Design, Synthesis and Biological Evaluation of Novel Benzoylimidazole Derivatives as Raf and Histone Deacetylases Dual Inhibitors [J] . Chen Xin, Gong Guoliang, Chen Xinyang, Chemical and Pharmaceutical Bulletin . 2019,第10期

机译：新型苯甲酰基咪唑衍生物的设计，合成及生物学评价为RAF和组蛋白脱乙酰酶双抑制剂
4. Synthesis, Evaluation and Molecular Modeling Study of L-2-amino-7/8-Bromoalkanoic Acid Derivatives as Histone Deacetylase Inhibitors [C] . Dawei Huang, Xiaohui Li, Zhilong Xiu, Chinese international peptide symposium . 2011

机译：L-2-氨基-7 / 8-溴烷酸衍生物作为组蛋白脱乙酰酶抑制剂的合成，评价和分子建模研究
5. Syntheses and biological evaluation of polyamine derivatives as histone deacetylase inhibitors. [D] . Varghese, Sheeba. 2006

机译：多胺衍生物作为组蛋白脱乙酰基酶抑制剂的合成及生物学评价。
6. Design Synthesis and Biological Evaluation of Novel Coumarin-Based Hydroxamate Derivatives as Histone Deacetylase (Hdac) Inhibitors with Antitumor Activities [O] . Feifei Yang, Na Zhao, Jiali Song, 2019

机译：新型基于香豆素的异羟肟酸酯衍生物作为具有抗肿瘤活性的组蛋白脱乙酰基酶（Hdac）抑制剂的设计合成和生物学评估
7. Design, Synthesis and Biological Evaluation of Nitro Oxide Donating N-Hydroxycinnamamide Derivatives as Histone Deacetylase Inhibitors [O] . Shiliang Tu, Hang Yuan, Jie Hu, 2014

机译：将硝基氧化物的设计，合成和生物学评价为组蛋白脱乙酰酶抑制剂作为组蛋白氧化氨基酰胺衍生物
8. Combinations of Novel Histone Deacetylase and Bcr-Abl Inhibitors in the Therapy of Imatinib Mesylate-Sensitive and -Refractory Bcr-Abl Expressing Leukemia [R] . Bhalla, K. 2008

机译：新型组蛋白去乙酰化酶和Bcr-abl抑制剂联合治疗伊马替尼甲磺酸盐敏感和难治性Bcr-abl表达白血病

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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