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Chinese Journal of Organic Chemistry >

2022 , Vol. 42 >Issue 2: 590 - 599

DOI: https://doi.org/10.6023/cjoc202107049

ARTICLES

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

  • Yaquan Cao ,
  • Yingxue Yang ,
  • Hongjin Zhai ,
  • Jin Wang ,
  • Shuo Zhang ,
  • Huanhuan Wang ,
  • Pu Yang ,
  • Chunli Wu
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  • 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
* Corresponding author. E-mail:

Received date: 2021-07-24

  Revised date: 2021-09-08

  Online published: 2022-02-24

Supported by

National Key Research and Development Project of China(2017YFD0501400)

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Abstract

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

Cite this article

Yaquan Cao , Yingxue Yang , Hongjin Zhai , Jin Wang , Shuo Zhang , Huanhuan Wang , Pu Yang , Chunli Wu . Synthesis and Antitumor Activity of Novel 5- and 6-Substituted Indazole Derivatives[J]. Chinese Journal of Organic Chemistry, 2022 , 42(2) : 590 -599 . DOI: 10.6023/cjoc202107049

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