一种 9-氮杂蒽并吡唑衍生物的缺氧激活前药，具有有前景的抗癌活性。

Hypoxia activated prodrugs of a 9-aza-anthrapyrazole derivative that has promising anticancer activity.

机构信息

Center for Drug Design and Development, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, Toledo, Ohio 43606, United States.

出版信息

J Med Chem. 2011 Dec 8;54(23):8224-7. doi: 10.1021/jm200984x. Epub 2011 Nov 4.

DOI:10.1021/jm200984x

PMID:22011244

Abstract

Mono- and bis-N-oxides of a 9-aza-anthrapyrazole derivative having two 2-(dimethylamino)ethyl appendages were prepared by using a mild oxaziridine reagent. Biochemical and cell culture assays indicate that the bis-oxide is an inactive prodrug that readily converts to the active parent molecule under hypoxic conditions that are analogous to those present within certain tumors.

摘要

用温和的氮氧化物试剂制备了具有两个 2-（二甲基氨基）乙基附加物的 9-氮杂蒽并吡唑衍生物的单-和双-N-氧化物。生化和细胞培养试验表明，双氧化物是一种无活性的前药，在类似于某些肿瘤中存在的缺氧条件下，很容易转化为活性母体分子。