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抗癌先导化合物JS-K的结构类似物的合成及其体外抗白血病活性

Synthesis and in vitro anti-leukemic activity of structural analogues of JS-K, an anti-cancer lead compound.

作者信息

Chakrapani Harinath, Goodblatt Michael M, Udupi Vidya, Malaviya Swati, Shami Paul J, Keefer Larry K, Saavedra Joseph E

机构信息

Chemistry Section, Laboratory of Comparative Carcinogenesis, National Cancer Institute at Frederick, PO Box B, Frederick, MD 21702, USA.

出版信息

Bioorg Med Chem Lett. 2008 Feb 1;18(3):950-3. doi: 10.1016/j.bmcl.2007.12.044. Epub 2008 Jan 4.

Abstract

Structural analogues of JS-K, an anti-cancer lead compound, were prepared and their in vitro anti-leukemic activity was determined. The rate of nitric oxide release from the corresponding diazeniumdiolate anions did not appear to affect the anti-leukemic activity of the prodrug forms. Two compounds with potent inhibitory activity and a potentially favorable toxicological profile were identified.

摘要

制备了抗癌先导化合物JS-K的结构类似物,并测定了它们的体外抗白血病活性。相应的二氮烯二醇盐阴离子释放一氧化氮的速率似乎不影响前药形式的抗白血病活性。鉴定出两种具有强效抑制活性和潜在良好毒理学特征的化合物。

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