2. Academic Validation
  3. Synthesis and antitumor activities of novel thiourea α-aminophosphonates from dehydroabietic acid

Synthesis and antitumor activities of novel thiourea α-aminophosphonates from dehydroabietic acid

  • Eur J Med Chem. 2013 Nov:69:508-20. doi: 10.1016/j.ejmech.2013.08.055.
Xiao-Chao Huang 1,  Meng Wang,  Ying-Ming Pan,  Gui-Yang Yao,  Heng-Shan Wang,  Xiao-Yan Tian,  Jiang-Ke Qin,  Ye Zhang
Affiliations

Affiliation

  • 1 State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Chemical Engineering of Guangxi Normal University, Yucai Road 15, Guilin 541004, Guangxi, PR China.
PMID: 24095745 DOI: 10.1016/j.ejmech.2013.08.055
Abstract

A series of novel thiourea α-aminophosphonate derivatives containing DHA structure was designed and synthesized as antitumor agents. Their inhibitory activities against the NCI-H460 (lung), A549 (lung adenocarcinoma), HepG2 (liver) and SKOV3 (ovarian) human Cancer cell lines were estimated using MTT assay in vitro. The screening results revealed that many compounds exhibited moderate to high levels of antitumor activities against the tested Cancer cell lines and that most demonstrated more potent inhibitory activities compared with the commercial Anticancer drug 5-fluorouracil. The mechanism of compound 5f was preliminarily investigated by acridine orange/ethidium bromide staining, Hoechst 33258 staining, JC-1 mitochondrial membrane potential staining, TUNEL assay, DNA ladder assay and flow cytometry, which indicated that the compound can induce cell Apoptosis in A549 cells.

Keywords

Apoptosis; Cytotoxicity; Dehydroabietic acid; Thiourea; α-Aminophosphonate.

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