2. Academic Validation
  3. Synthesis and antitumor activities of novel dipeptide derivatives derived from dehydroabietic acid

Synthesis and antitumor activities of novel dipeptide derivatives derived from dehydroabietic acid

  • Bioorg Med Chem Lett. 2014 Mar 15;24(6):1511-8. doi: 10.1016/j.bmcl.2014.02.001.
Xiao-Chao Huang 1,  Meng Wang 1,  Heng-Shan Wang 1,  Zhen-Feng Chen 1,  Ye Zhang 2,  Ying-Ming Pan 3
Affiliations

Affiliations

  • 1 State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Pharmaceutical Science of Guangxi Normal University, Yucai Road 15, Guilin 541004, Guangxi, PR China.
  • 2 State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Pharmaceutical Science of Guangxi Normal University, Yucai Road 15, Guilin 541004, Guangxi, PR China; Department of Chemistry & Pharmaceutical Science, Guilin Normal College, Xinyi Road 15, Guangxi 541001, PR China. Electronic address: zhangye81@126.com.
  • 3 State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Pharmaceutical Science of Guangxi Normal University, Yucai Road 15, Guilin 541004, Guangxi, PR China. Electronic address: panym2005@sina.com.
PMID: 24565905 DOI: 10.1016/j.bmcl.2014.02.001
Abstract

A series of dipeptide derivatives from dehydroabietic acid were designed and synthesized as novel antitumor agents. The antitumor activities screening indicated that many compounds showed moderate to high levels of inhibition activities against NCI-H460, HepG2, SK-OV-3, BEL-7404, HeLa and HCT-116 Cancer cell lines and that some displayed more potent inhibitory activities than commercial Anticancer drug 5-fluorouracil. The mechanism of representative compound 7b was studied by AO/EB staining, Hoechst 33258 staining, JC-1 mitochondrial membrane potential staining, TUNEL assay, DNA ladder assay and flow cytometry, which exhibited that the compound could induce Apoptosis in HeLa cells. Further investigation showed that compound 7b induced Apoptosis of HeLa cells through a mitochondrial pathway.

Keywords

Apoptosis; Cytotoxicity; Dehydroabietic acid; Dipeptide.

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