Design, Synthesis, and Preliminary Bioactivity Evaluation of 2,7-Substituted Carbazole Derivatives as Potent Autotaxin Inhibitors and Antitumor Agents

Wang Wenming; Zhao Fengmei; Zhao Yarui; Pan Weiwei; Cao Pengcheng; Wu Lintao; Wang Zhijun; Zhao Xuan; Zhao Yi; Wang Hongfei

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Design, Synthesis, and Preliminary Bioactivity Evaluation of 2,7-Substituted Carbazole Derivatives as Potent Autotaxin Inhibitors and Antitumor Agents

机译：2,7取代的咔唑衍生物作为有效的自坦蛋白抑制剂和抗肿瘤剂的设计，合成和初步生物活性评价

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Background: Autotaxin-LPA signaling has been implicated in cancer progression, and targeted for the discovery of cancer therapeutic agents.

机译：背景：自身XIN-LPA信号传导与癌症进展有关，并针对发现癌症治疗剂的发现。

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《Nature reviews Cancer》 |2019年第2期|共9页
作者
Wang Wenming; Zhao Fengmei; Zhao Yarui; Pan Weiwei; Cao Pengcheng; Wu Lintao; Wang Zhijun; Zhao Xuan; Zhao Yi; Wang Hongfei;
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作者单位

Biol Inst Shanxi Taiyuan 030006 Shanxi Peoples R China;

Biol Inst Shanxi Taiyuan 030006 Shanxi Peoples R China;

Biol Inst Shanxi Taiyuan 030006 Shanxi Peoples R China;

Biol Inst Shanxi Taiyuan 030006 Shanxi Peoples R China;

Biol Inst Shanxi Taiyuan 030006 Shanxi Peoples R China;

Changzhi Univ Dept Chem Changzhi 046011 Shanxi Peoples R China;

Changzhi Univ Dept Chem Changzhi 046011 Shanxi Peoples R China;

Univ Memphis Dept Chem Memphis TN 38152 USA;

Biol Inst Shanxi Taiyuan 030006 Shanxi Peoples R China;

Shanxi Univ Inst Mol Sci Kev Lab Chem Biol &

Mol Engn Educ Minist Taiyuan 030006 Shanxi;

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原文格式 PDF
正文语种 eng
中图分类肿瘤学;
关键词
Autotaxin; carbazole derivatives; phosphodiesterase inhibitor; cytotoxicity; anticancer drug; molecular docking;

机译：自身X蛋白;咔唑衍生物;磷酸二酯酶抑制剂;细胞毒性;抗癌药物;分子对接;

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1. Design, Synthesis, and Preliminary Bioactivity Evaluation of 2,7-Substituted Carbazole Derivatives as Potent Autotaxin Inhibitors and Antitumor Agents [J] . Wang Wenming, Zhao Fengmei, Zhao Yarui, Nature reviews Cancer . 2019,第2期

机译：2,7取代的咔唑衍生物作为有效的自坦蛋白抑制剂和抗肿瘤剂的设计，合成和初步生物活性评价
2. Design, synthesis, biological evaluation and preliminary mechanism study of novel benzothiazole derivatives bearing indole-based moiety as potent antitumor agents [J] . Ma Junjie, Bao Guanglong, Wang Limei, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2015,第Null期

机译：以吲哚基部分为有效抗肿瘤剂的新型苯并噻唑衍生物的设计，合成，生物学评价和初步机理研究
3. Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents [J] . Li Zhang, Wang Zhong-Chang, Li Xin, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2019,第期

机译：新型二芳基-1,5-二氮杂衍生物的设计，合成和评价载体吗啉，富含二核COX-2/5-LOX抑制剂和抗肿瘤剂
4. Design, Synthesis and evaluation of novel 1,3,4-thiadiazole derivatives as potent anticonvulsant agents with lesser neurotoxicity. [C] . Abhilasha Verma, Manoj kumar Annual meeting exposition of the Controlled Release Society . 2011

机译：设计，合成和评估新型1,3,4-噻二唑衍生物作为有效的抗惊厥药，具有较小的神经毒性。
5. Design, synthesis, and biological evaluation of betulinic acid derivatives as potent anti-HIV-1 agents. [D] . Qian, Keduo. 2008

机译：作为有效的抗HIV-1药物的桦木酸衍生物的设计，合成和生物学评估。
6. Antitumor Agents 266*. Design Synthesis and Biological Evaluation of Novel 2-(Furan-2-yl) naphthalen-1-ol Derivatives as Potent and Selective Anti-Breast Cancer Agents [O] . Yizhou Dong, Qian Shi, Yi-Nan Liu, -1

机译：抗肿瘤药物266 *。新颖的设计合成和生物学评价2-（呋喃-2-基）萘-1-醇衍生物作为有效且选择性的抗乳腺癌试剂
7. Design, synthesis, biological evaluation and preliminary mechanism study of novel benzothiazole derivatives bearing indole-based moiety as potent antitumor agents [O] . Junjie Ma, Guanglong Bao, Limei Wang, 2015

机译：新型苯并噻唑衍生物的设计，合成，生物学评价及初步机制研究，其吲哚基部分作为有效抗肿瘤剂

Design, Synthesis, and Preliminary Bioactivity Evaluation of 2,7-Substituted Carbazole Derivatives as Potent Autotaxin Inhibitors and Antitumor Agents

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