Chinese Journal of Organic Chemistry ›› 2022, Vol. 42 ›› Issue (2): 590-599.DOI: 10.6023/cjoc202107049 Previous Articles     Next Articles

ARTICLES

新型5位与6位取代的吲唑类衍生物的合成及抗肿瘤活性研究

曹亚权a,b, 杨莹雪a,b, 翟洪进a,b, 王锦a,b, 张烁a,b, 王焕焕a,b, 杨璞a,b, 吴春丽a,b,c,*()   

  1. a 郑州大学药学院 郑州 450001
    b 新药创制与药物安全性评价河南省协同创新中心 郑州 450001
    c 教育部药物关键制备技术重点实验室 郑州 450001
  • 收稿日期:2021-07-24 修回日期:2021-09-08 发布日期:2022-02-24
  • 通讯作者: 吴春丽
  • 基金资助:
    国家重点研究开发(2017YFD0501400)

Synthesis and Antitumor Activity of Novel 5- and 6-Substituted Indazole Derivatives

Yaquan Caoa,b, Yingxue Yanga,b, Hongjin Zhaia,b, Jin Wanga,b, Shuo Zhanga,b, Huanhuan Wanga,b, Pu Yanga,b, Chunli Wua,b,c()   

  1. a School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001
    b Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou 450001
    c Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou 450001
  • Received:2021-07-24 Revised:2021-09-08 Published:2022-02-24
  • Contact: Chunli Wu
  • Supported by:
    National Key Research and Development Project of China(2017YFD0501400)

In order to search for new antitumor drugs with high efficiency and low toxicity, 5- and 6-substituted indazole compounds were designed and synthesized. The antiproliferative activity of target compounds in four human cancer cells, PC-3 (human prostate cancer cell), MCF-7 (human breast cancer cell), HepG-2 (human hepatoma cell) and MGC-803 (human gastric cancer cell), was evaluated by thiazole blue (MTT) method. The results showed that most of the compounds had specific antiproliferative activity against PC-3. Among them, N-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)-1-isopropyl-1H-in- doleazole-5-carboxyamide (8a) and N-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)-1-isopropyl-1H-indoleazole-6-formamide (14a) possess strong antitumor activity against PC-3 with IC50 values of 6.21 and 6.43 μmol/L, respectively. It provides a new idea for the research of anti-tumor drugs for prostate cancer.

Key words: indazole, cancer, antiproliferative activity, prostatic cancer