DESIGN, SYNTHESIS, AND ANTI-INFLAMMATORY ACTIVITY OF NOVEL 20-<i>O</i>-SUBSTITUTED CAMPTOTHECIN CARBAMATE DERIVATIVES
Keywords:
camptothecin, carbamate, anti-inflammatory activity, drug designAbstract
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).
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Published
2024-08-01
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Original Papers