The synthesis, structural study and anticancer activity evaluation of emodin derivatives containing conjugative groups.

Abstract

Eight new emodin derivatives that contain large conjugative system have been synthesized and their anticancer activities also have been evaluated. The result shows that large conjugative system can not enhance the anticancer activities of emodin derivatives, but the introduction of an alkylating center can make emodin derivative effective against cancer cell lines. Compound 12 has the highest alkylating ability, but its anticancer activity is not remarkable, which indicates that there is not a direct correlation between the chemical reactivity of the alkylating agent and the toxic effects.

• Authors: Wang Wen-Feng, Zhang Feng-Sen, Zhao Wen-Na, Bai Ze-Dong, Yang Hui-Jun, Shao Jing-Wei, Yuan Yao-Feng
• Journal: Medicinal chemistry (Shariqah (United Arab Emirates)) (Med Chem) Vol. 9 Issue 4 Pg. 545-52 (Jun 01 2013) ISSN: 1875-6638 [Electronic] Netherlands
• PMID: 22920154 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Antineoplastic Agents, Alkylating
• Emodin

Topics

• Antineoplastic Agents (chemical synthesis, pharmacology)
• Antineoplastic Agents, Alkylating (chemical synthesis, pharmacology)
• Cell Proliferation (drug effects)
• Cell Survival (drug effects)
• Dose-Response Relationship, Drug
• Drug Screening Assays, Antitumor
• Emodin (analogs & derivatives, chemical synthesis, pharmacology)
• Humans
• Structure-Activity Relationship
• Tumor Cells, Cultured