کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1395302 | 1501204 | 2009 | 10 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Novel derivatives of 6-mercaptopurine: Synthesis, characterization and antiproliferative activities of S-allylthio-mercaptopurines Novel derivatives of 6-mercaptopurine: Synthesis, characterization and antiproliferative activities of S-allylthio-mercaptopurines](/preview/png/1395302.png)
Biologically active S-allylthio derivatives of 6-mercaptopurine (6-MP) and 6-mercaptopurine riboside (6-MPR) were synthesized. The products, S-allylthio-6-mercaptopurine (SA-6MP) and S-allylthio-6-mercaptopurine riboside (SA-6MPR) were characterized. The antiproliferative activity of the new prodrugs was tested on human leukemia and monolayer cell lines, and compared to that of their parent reactants. The new prodrugs acted by a concentration-dependent mechanism. They inhibited cell proliferation and induced-apoptosis more efficiently than the parent molecules. Leukemia cell lines were more sensitive to the new prodrugs than monolayer cell lines. Higher hydrophobicity of the derivatives improves their penetration into cells, where upon reaction with glutathione, S-allylthioglutathione (GSSA) is formed, and 6-MP or 6-MPR is released for further processing.
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Journal: European Journal of Medicinal Chemistry - Volume 44, Issue 2, February 2009, Pages 541–550