Related Experiment Video
Updated: Jun 14, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Phosphate ester derivatives of homocamptothecin: synthesis, solution stabilities and antitumor activities
Zhenyuan Miao1, Jing Zhang, Liang You
1School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China.
Abstract:
Homocamptothecins (hCPTs) represents a new promising class of topoisomerase I inhibitors with enhanced stability and superior antitumor activity. Some phosphodiesters and phosphotriesters homocamptothecin derivatives were designed and synthesized based on our previous synthetic route. The cytotoxicity in vitro on three cancer cell lines and antitumor activity in vivo, and inhibitory properties of topoisomerase I of these derivatives were evaluated. Among them compounds 24e and 24f exhibited higher cytotoxic activity than IRT and the former exhibited the best antitumor activity in vivo and solution stability both at pH 7.4 and pH 3.0.
More Related Videos
Related Concept Videos
Drugs that Destabilize Microtubules
Drugs that Stabilize Microtubules
Pharmaceutical Alternatives: Stability-Related Therapeutic Nonequivalence
Antifungal Agents
Antiviral Nucleoside Inhibitors
Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence

