Synthesis and antitumor activity of 5'-deoxy-4'-thio-L-nucleosides
Liqing Cong1, Weicheng Zhou, Dongzhe Jin
1State Key Laboratory of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, 1111 Zhongshanbeiyi Road, Shanghai 200437, China. cong75@139.com
Abstract:
A series of novel 5'-deoxy-4'-thio-L-nucleosides was designed and synthesized. The absolute configuration of the target compound 23alpha was confirmed by X-ray crystallography. The antitumor activities of the target compounds were tested against the growth of human carcinoma of colon (LOVO), human leukemia cell line (CEM) and human breast cancer cell line (MDA-MB-435) cells in vitro. 6-cyclopentylamino and 6-cyclohexylamino purine compounds 26 and 27, both in alpha-configuration and in beta-form, exhibited strong inhibition to CEM.
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