State Key Laboratory of Virology, College of Chemistry and Molecular Sciences, Wuhan University, Wuhan, PR China.
Bioorg Med Chem Lett. 2010 Oct 15;20(20):5979-83. doi: 10.1016/j.bmcl.2010.08.093. Epub 2010 Aug 21.
Novel arylethynyltriazole acyclonucleosides were synthesized and assessed for their anticancer activity on drug-resistant pancreatic cancer MiaPaCa-2 cells. One lead compound was found to have much more potent apoptosis-related antiproliferative effects than gemcitabine, the current first-line treatment for pancreatic cancer. Further investigations showed that this active compound did not inhibit DNA synthesis, which means that it does not resemble gemcitabine and may involve a different mechanism of action.
新型芳基乙炔三氮唑环核苷类似物被合成并评估了它们对耐药性胰腺癌 MiaPaCa-2 细胞的抗癌活性。发现一种先导化合物具有比当前用于胰腺癌一线治疗的吉西他滨更强的凋亡相关抗增殖作用。进一步的研究表明，这种活性化合物不抑制 DNA 合成，这意味着它与吉西他滨不同，可能涉及不同的作用机制。
