DESIGN, SYNTHESIS, AND ANTI-INFLAMMATORY ACTIVITY OF NOVEL 20-<i>O</i>-SUBSTITUTED CAMPTOTHECIN CARBAMATE DERIVATIVES

Authors

  • Yazhao Zhu School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418
  • Chuanhao Wang Key Laboratory for Soft Chemistry and Functional Materials, Ministry of Education, Nanjing University of Science and Technology, Nanjing 210094
  • Rongxue Lv School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418
  • Hang Yang School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418
  • Yongchang Wang School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418
  • Yuelin Wu School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418

Keywords:

camptothecin, carbamate, anti-inflammatory activity, drug design

Abstract

Twelve novel camptothecin derivatives with a carbamate substituent at position 20 were designed and synthesized. Most of the targeted compounds indicated potent anti-inflammatory activity in a lipopolysaccharide stimulation of peritoneal macrophage model. Among them, the benzyl(methyl)amine derivative showed the most pronounced anti-inflammatory activity at a concentration of 1 μM and TNF-α inhibitory rate is increased by 10.2% compared to the lead compound (N,N-dimethylethylenediamine derivative).

Author Biographies

Yazhao Zhu, School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418

School of Chemical and Environmental Engineering, M.S.

Chuanhao Wang, Key Laboratory for Soft Chemistry and Functional Materials, Ministry of Education, Nanjing University of Science and Technology, Nanjing 210094

Key Laboratory for Soft Chemistry and Functional Materials, Ministry of Education, PhD

Rongxue Lv, School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418

School of Chemical and Environmental Engineering, M.S.

Hang Yang, School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418

School of Chemical and Environmental Engineering, M.S.

Yongchang Wang, School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418

School of Chemical and Environmental Engineering, M.S.

Yuelin Wu, School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418

School of Chemical and Environmental Engineering, Prof.

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Published

2024-08-01

Issue

Vol. 60 No. 5/6 (2024)

Section

Original Papers