5'-脱氧-4'-硫代-L-核苷的合成及抗肿瘤活性。

Synthesis and antitumor activity of 5'-deoxy-4'-thio-L-nucleosides.

机构信息

State Key Laboratory of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, 1111 Zhongshanbeiyi Road, Shanghai 200437, China.

出版信息

Chem Biol Drug Des. 2010 Jun;75(6):619-27. doi: 10.1111/j.1747-0285.2010.00967.x. Epub 2010 Mar 23.

DOI:10.1111/j.1747-0285.2010.00967.x

PMID:20337785

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.

摘要

设计并合成了一系列新型的 5'-脱氧-4'-硫代-L-核苷。通过 X 射线晶体学确定了目标化合物 23alpha 的绝对构型。测试了目标化合物对体外人结肠癌细胞（LOVO）、人白血病细胞系（CEM）和人乳腺癌细胞系（MDA-MB-435）生长的抗肿瘤活性。6-环戊基氨基和 6-环己基氨基嘌呤化合物 26 和 27，无论是在 alpha-构型还是 beta-形式，都对 CEM 表现出强烈的抑制作用。