A broad spectrum anticancer nucleoside with selective toxicity against human colon cells in vitro

作者：Shelton Jadd R; Burt Scott R; Peterson Matt A^*

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(5): 1484-1487.

DOI：10.1016/j.bmcl.2011.01.003

• Purine nucleosides
• Bio-active adenosine derivatives
• Antiproliferative nucleosides

2',3'-Bis-O-tert-butyldimethylsilyl-5'-deoxy-5'-[N-(methylcarbamoyl)amino]-N-6-(N-phenylcarbamoyl)-adenosine, a new member of the N-6,5'-bis-ureidoadenosine class of anticancer nucleosides, is found to exhibit broad spectrum antiproliferative activity. A majority of the cell lines in the NCI-60 are inhibited with an average GI(50) = 3.13 mu M. Selective toxicity against human colon cancer cell lines (COLO 205, HCC-2998, HCT-116, HT29, KM12) was also exhibited (LC50' s = 6-10 mu M).

• 出版日期2011-3-1