3-酮安圭定的还原胺化反应及产物的抗肿瘤活性
Reductive amination of 3-ketoanguidin and antitumor activity of the products.
作者信息
Kaneko T, Wong H, Howell H G, Rose W C, Bradner W T, Doyle T W
出版信息
J Med Chem. 1985 Jul;28(7):958-60. doi: 10.1021/jm00145a019.
PMID:4009618
Abstract
Amine-containing trichothecanes were prepared by reductive aminations of 3-ketoanguidin. In in vivo tests against P388 leukemia, most of them showed an improved activity compared to anguidin though their potency was decreased. 3-Ketoanguidin also produced some unexpected structures: oxazoline 5, dioxalane 7, and alpha-amino nitrile 13.
摘要
含胺的单端孢霉烯族毒素是通过3-酮安圭定的还原胺化反应制备的。在针对P388白血病的体内试验中，尽管它们的效力有所降低，但大多数与安圭定相比显示出更高的活性。3-酮安圭定还产生了一些意想不到的结构：恶唑啉5、二氧戊环7和α-氨基腈13。
Zotero 插件