Design and Synthesis of 7-Azaindole Derivatives and Their Antitumor and Analgesic Activities

• Published in: Journal of the Chemical Society of Pakistan Vol. 42; no. 3; p. 460
• Main Authors: Xue Kun Liu, Xue Kun Liu, Yan Qiu Wang, Yan Qiu Wang, Tong Jian Zhao, Tong Jian Zhao, Yuan Hua Lu, Yuan Hua Lu, Jia Nan Zhao, Jia Nan Zhao, Xiao Yu Geng, Xiao Yu Geng, Jie Ma, Jie Ma
• Format: Journal Article
• Language: English
• Published: Knowledge Bylanes 30.06.2020
• Subjects: Analgesics
• ISSN: 0253-5106
• DOI: 10.52568/000641

To develop effective anti-tumor and analgesic drugs, a series of novel 7-azaindole derivatives were designed and synthesized through a four-step reaction. 18 target compounds were obtained and characterized through Nuclear Magnetic Resonance and High Resolution Mass Spectrometry. Their anti-proliferative activities and analgesic effect were evaluated. When the 1-position was a methylsulfonyl group and the 5-position was a nitro group, compound 4f demonstrated the best activity. Furthermore, there was a dramatic difference between the IC50 values of compound 4f in tumor and in healthy cell line. The IC50 values of compound 4f in MCF7 breast cancer cell line was 5.781 μmol/L and 8.077 μmol/L in HepG2 hepatoma carcinoma cell line, but more than 100 μmol/L in HL7702 liver cell line. Preliminary results showed that compounds 3a, 3g and 4i had significant analgesic effects in mice, which were stronger than aspirin. These compounds have good prospects for new drug development.