Novel 25-hydroxyprotopanaxadiol derivatives incorporating chloroacetyl chloride and their anti-tumor evaluation.

Abstract

In the current work, 12 novel 25-hydroxyprotopanaxadiol (25-OH-PPD) derivatives were synthesized by reacting with chloroacetyl chloride. And their in vitro antitumor activities were evaluated on six human tumor cell lines by MTT assay. The results demonstrated that, as compared with 25-OH-PPD, compounds 4, 6 and 7 exhibited higher cytotoxic activity on all tested cell lines. Of them, compound 4 showed strongly inhibition against MCF-7, HCT-116 and Lovo cells with IC50 values of 1.7, 1.6 and 2.1 μM, respectively. The IC₅₀ values of compound 6 against HCT-116 and 7 against MCF-7 were the lowest (1.2 and 1.6 μM, respectively). It was also noted that compound 4 showed a 20- to 100-fold greater growth inhibition than ginsenoside-Rg₃ (an anti-cancer regular drug in China). In conclusion, the data revealed that compounds 4, 6 and 7 were potential candidates for anti-tumor treatment and may be useful for the development of novel antiproliferative agents.

• Authors: Fan-Zhi Qu, Ya-Fei Liu, Jia-Qing Cao, Xu-De Wang, Xiao-Shu Zhang, Chen Zhao, Yu-Qing Zhao
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 24 Issue 23 Pg. 5390-4 (Dec 01 2014) ISSN: 1464-3405 [Electronic] England
• PMID: 25453794 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 25-hydroxyprotopanaxadiol
• Acetates
• Antineoplastic Agents
• Biological Products
• Ginsenosides
• chloroacetyl chloride

Topics

• Acetates (chemistry, metabolism)
• Antineoplastic Agents (pharmacology)
• Biological Products
• Cell Line, Tumor
• Cell Proliferation
• Ginsenosides (chemistry, metabolism)
• Humans
• Molecular Structure
• Neoplasms (drug therapy)
• Panax (chemistry)
• Structure-Activity Relationship