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Updated: Aug 17, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and antitumor activity of A-ring modified hexacyclic analogues of camptothecin
Di-zao Li1, Cun-ying Wang, Xian-dao Pan
1Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Vedical College, Beijing 100050, China.
Aim:
To improve the biological activity of A-ring modified analogues of camptothecin.
Methods:
A-ring modified camptothecins were synthesized from 10-hydroxycamptothecin or 7-ethyl-10-hydroxycamptothecin (SN-38) in three or four steps. Their cytotoxicity was evaluated using MTY assay, and their in vivo antitumnor activity against mouse liver cancer H22 was tested. Results Five hexacyclic camptothecins (6a, 6b, 6c, 7a and 7b) are target compounds, and ten camptothecin derivatives are new compounds.
Conclusion:
The modification of a 1,4-oxazine-2-one ring fused with positions 9 and 10 of A-ring will reduce the antitumor activity of camptothecins.
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