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Synthesis of Potential Anticancer 1-(1H-Indol-3-yl)isoquinolines by Silver Nitrate Mediated Tandem Reactions of 2-Alkynylbenzaldehyde Azines and Indoles
Synlett ( IF 1.7 ) Pub Date : 2018-01-02 , DOI: 10.1055/s-0036-1591743 Yun-Hui Zhao 1, 2 , Zhihua Zhou 1, 2 , Yong-Cheng Ma 3 , Yueyang Luo 1 , Yingli Zhu 3 , Hang Wang 1 , Hangbin Zhou 1 , Hailong Tan 1 , Wenlin Xie 1, 2 , Zilong Tang 4
Synlett ( IF 1.7 ) Pub Date : 2018-01-02 , DOI: 10.1055/s-0036-1591743 Yun-Hui Zhao 1, 2 , Zhihua Zhou 1, 2 , Yong-Cheng Ma 3 , Yueyang Luo 1 , Yingli Zhu 3 , Hang Wang 1 , Hangbin Zhou 1 , Hailong Tan 1 , Wenlin Xie 1, 2 , Zilong Tang 4
Affiliation
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Novel antitumor compounds featuring isoquinoline and indole moieties were synthesized by a silver nitrate promoted domino reaction involving intramolecular cyclization, nucleophilic addition of indole, and subsequent N–N bond cleavage. The transformation from readily available starting materials into an interesting class of indole-substituted isoquinolines was completed under mild conditions and by simple operations in moderate to good yields. The antitumor activity of these compounds in vitro was significantly greater than that of a reference compound, 5-fluorouracil. The products might serve as new lead compounds for drugs for the treatment of cancer.
中文翻译：
通过硝酸银介导的 2-炔基苯甲醛吖嗪和吲哚的串联反应合成潜在的抗癌 1-(1H-Indol-3-yl)isoquinolines
通过硝酸银促进的多米诺反应合成了具有异喹啉和吲哚部分的新型抗肿瘤化合物，包括分子内环化、吲哚的亲核加成和随后的 N-N 键断裂。从容易获得的原料到一类有趣的吲哚取代异喹啉的转化是在温和的条件下通过简单的操作以中等至良好的产率完成的。这些化合物的体外抗肿瘤活性显着高于参考化合物 5-氟尿嘧啶。这些产品可作为治疗癌症药物的新先导化合物。
更新日期：2018-01-02
中文翻译：
通过硝酸银介导的 2-炔基苯甲醛吖嗪和吲哚的串联反应合成潜在的抗癌 1-(1H-Indol-3-yl)isoquinolines
通过硝酸银促进的多米诺反应合成了具有异喹啉和吲哚部分的新型抗肿瘤化合物，包括分子内环化、吲哚的亲核加成和随后的 N-N 键断裂。从容易获得的原料到一类有趣的吲哚取代异喹啉的转化是在温和的条件下通过简单的操作以中等至良好的产率完成的。这些化合物的体外抗肿瘤活性显着高于参考化合物 5-氟尿嘧啶。这些产品可作为治疗癌症药物的新先导化合物。
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