2-氰基-28-羟基-羽扇-1-烯-3-酮的合成及其细胞毒性
Synthesis and cytotoxicity of 2-cyano-28-hydroxy-lup-1-en-3-ones.
作者信息
Koohang Ali, Majewski Nathan D, Szotek Erika L, Mar Aye Aye, Eiznhamer David A, Flavin Michael T, Xu Ze-Qi
机构信息
Advanced Life Sciences, Inc, Research and Development, Woodridge, IL 60517, USA.
出版信息
Bioorg Med Chem Lett. 2009 Apr 15;19(8):2168-71. doi: 10.1016/j.bmcl.2009.02.107. Epub 2009 Mar 3.
PMID:19286375
Abstract
New A-ring modified betulin and dihydrobetulin derivatives possessing the 2-cyano-1-en-3-one moiety were prepared and tested for cytotoxicity in seven cancer cell lines. The most active agent 9a synthesized in this account was further demonstrated to induce apoptosis and to activate caspases in malignant melanoma cells.
摘要
制备了具有2-氰基-1-烯-3-酮部分的新型A环修饰桦木醇和二氢桦木醇衍生物，并在七种癌细胞系中测试了它们的细胞毒性。本文合成的活性最高的试剂9a进一步证明可诱导恶性黑色素瘤细胞凋亡并激活半胱天冬酶。
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