合成三种不同二糖通过 15-位羟基连接的 5(6)-二氢 OSW-1 类似物及其抗肿瘤活性。
Synthesis of 5(6)-dihydro-OSW-1 analogs bearing three kinds of disaccharides linking at 15-hydroxy and their antitumor activities.
机构信息
Key Laboratory of Bioactivity Substance and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Peking 100050, PR China.
出版信息
Bioorg Med Chem Lett. 2011 May 15;21(10):2921-4. doi: 10.1016/j.bmcl.2011.03.065. Epub 2011 Mar 23.
In order to study the SAR of 5(6)-dihydro-OSW-1, eight 15(α)β-O-glycosyl analogs (26-33) carrying three kinds of disaccharides including [β-d-Xylp-(1-3)-α-l-Arap], [β-d-Xylp-(1-4)-α-l-Arap] and [α-l-Rhap-(1-2)-(α)β-d-Glcp] were designed and synthesized. Their in vitro antitumor activities were tested by the standard MTT assay which disclosed that compound 33 (IC(50)=0.28-0.52 μM) showed potential antitumor activities.
为了研究 5(6)-二氢 OSW-1 的 SAR，设计并合成了 8 种带有三种二糖的 15(α)β-O-糖苷类似物（26-33），包括 [β-d-Xylp-(1-3)-α-l-Arap]、[β-d-Xylp-(1-4)-α-l-Arap] 和 [α-l-Rhap-(1-2)-(α)β-d-Glcp]。采用标准 MTT 法测定其体外抗肿瘤活性，结果表明化合物 33（IC(50)=0.28-0.52 μM）具有潜在的抗肿瘤活性。
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