Design, synthesis, and biological activity evaluation of campthothecin-HAA-Norcantharidin conjugates as antitumor agents in vitro

Xian H Wang; Mei Huang; Chang K Zhao; Chan Li; Lang Xu

doi:10.1111/cbdd.13397

Design, synthesis, and biological activity evaluation of campthothecin-HAA-Norcantharidin conjugates as antitumor agents in vitro

Chem Biol Drug Des. 2019 Jun;93(6):986-992. doi: 10.1111/cbdd.13397. Epub 2018 Oct 31.

Authors

Xian H Wang¹, Mei Huang², Chang K Zhao¹, Chan Li³, Lang Xu¹

Affiliations

¹ School of Pharmacy, Zunyi Medical University, Zunyi City, Guizhou Province, China.
² Department of Pharmacology and Key Laboratory of Basic Pharmacology of Ministry of Education, Zunyi Medical University, Zunyi City, Guizhou Province, China.
³ School of Pharmacy, Sun Yat-Sen University, Guangzhou, Guangdong Province, China.

PMID: 30218487
DOI: 10.1111/cbdd.13397

Abstract

Three components of Camptothecin, hydroxyacetic acid, and functionalized norcantharidins were constructed together to form a novel series of camptothecin derivatives in a good yield. The synthesized campthothecin-HAA-norcantharidin conjugate pro-drugs could suppress cancer cell growth in vitro. These conjugated pro-drug molecules possess therapeutic potential as novel bi-functional conjugates platforms for cancer treatment.

Keywords: camptothecin; conjugate; hydroxyacetic acid; norcantharidin; pro-drug.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents, Phytogenic / chemical synthesis
Antineoplastic Agents, Phytogenic / chemistry
Antineoplastic Agents, Phytogenic / pharmacology*
Bridged Bicyclo Compounds, Heterocyclic / chemistry
Bridged Bicyclo Compounds, Heterocyclic / pharmacology*
Camptothecin / chemistry
Camptothecin / pharmacology*
Cell Line, Tumor
Drug Design*
Drug Screening Assays, Antitumor
Humans

Substances

Antineoplastic Agents, Phytogenic
Bridged Bicyclo Compounds, Heterocyclic
norcantharidin
Camptothecin