کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1369544 | 981781 | 2016 | 5 صفحه PDF | دانلود رایگان |
A group of podophyllotoxin (PPT) derivatives (7a–j) were synthesized by conjugating aryloxyacetanilide moieties to the 4′-hydroxyl of 4′-demethyl-4-deoxypodophyllotoxin (DDPT), and their anticancer activity was evaluated. It was found that the most potent compound 7d inhibited the proliferation of three cancer cell lines with sub to low micromolar IC50 values. Furthermore, it was demonstrated that 7d induced cell cycle arrest in G2/M phase in MGC-803 cells, and regulated the expression of cell cycle check point proteins, such as cyclin A, cyclin B, CDK1, cdc25c, and p21. Finally, 4 mg/kg of 7d reduced the weights and volumes of HepG2 xenografts in mice. Our findings suggest that 7d might be a potential anticancer agent.
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Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 4, 15 February 2016, Pages 1360–1364