Pyrimidoquinazoline-based antitumor agents. Design of topoisomerase II to DNA cross-linkers with activity against protein kinases
…, X Huang, R Martinez, RH Lemus…
Index: Skibo, Edward B.; Huang, Xiaofen; Martinez, Rogelio; Lemus, Robert H.; Craigo, William A.; Dorr, Robert T. Journal of Medicinal Chemistry, 2002 , vol. 45, # 25 p. 5543 - 5555
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Citation Number: 34
Abstract
A series of pyrimidoquinazoline analogues, possessing either 4, 5-g or 5, 4-g fusion, were studied with respect to cytotoxicity, topoisomerase II inhibitory activity, in vivo activity, and DNA cleavage and DNA-protein cross-linking properties. These analogues were designed as electron-deficient anthraquinones with dual alkylating centers to cross-link DNA with topoisomerase II. Our studies verified the presence of DNA-protein cross-linking in vitro as ...
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