SYNTHESIS <i>VIA</i> THE MANNICH REACTION AND BIOLOGICAL ACTIVITY OF NOVEL FLUORINATED CAMPTOTHECIN DERIVATIVES

Authors

  • Chuanhao Wang School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418, China
  • Yuan Wang School of Pharmacy, Ningxia Medical University, 1160 Shengli St., Yinchuan, Ningxia 750004, China
  • Haijun Ma School of Pharmacy, Ningxia Medical University, 1160 Shengli St., Yinchuan, Ningxia 750004, China
  • Yazhao Zhu School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418, China
  • Yanming Zhang School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China
  • Zhenyuan Miao School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China
  • Yuelin Wu School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai 201418, China

DOI:

https://doi.org/10.1007/6038

Keywords:

fluorinated camptothecin, antitumor activity, Mannich reaction, natural products.

Abstract

Two series of fluorinated camptothecin derivatives had been designed and synthesized via the Mannich reaction. The hexacyclic fluorinated camptothecin derivatives were found to be more active. (9S,10S)-2-Cyclopropyl-9-ethyl-10-fluoro-9-hydroxy-2,3,9,10,12,15-hexahydro-1H,13H-[1,3]oxazino[5,6-f]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-13-one showed potent antitumor activity against A549 and T24 cell lines with effective topoisomerase I inhibitory activity.

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Published

2021-06-19

Issue

Vol. 57 No. 6 (2021)

Section

Short Communications