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    Synthesis of quinobenzoxazine analogues with topoisomerase II and quadruplex interactions for use as antineoplastic agents
    17.
    发明授权
    Synthesis of quinobenzoxazine analogues with topoisomerase II and quadruplex interactions for use as antineoplastic agents 失效
    合成具有拓扑异构酶II和四联体相互作用的喹诺酮类似物用作抗肿瘤剂

    公开(公告)号：US06528517B1

    公开(公告)日：2003-03-04

    申请号：US09245019

    申请日：1999-02-04

    Applicant: Laurence H. Hurley ,  Qingping Zeng ,  Yan Kwok ,  Jongsik Gam ,  Sean M. Kerwin

    Inventor： Laurence H. Hurley ,  Qingping Zeng ,  Yan Kwok ,  Jongsik Gam ,  Sean M. Kerwin

    IPC: A61K3144

    CPC classification number: C07D498/06 ,  C07D498/16

    Abstract: The present invention discloses a novel quinobenzoxazine self-assembly complex on DNA and on the topoisomerase II-DNA complex. The related model is used to design a new series of quinobenzoxazines, pyridobenzophenoxazines, pyrridonaphthophenoxazines, and other related compounds that may exhibit anticancer or antibiotic activity. The anticancer activity of these compounds is thought to operate via stabilization of the topoisomerase II-DNA complex and/or interaction with G-quadruplexes, while the antibiotic activity of these compounds derives from their ability to inhibit gyrase, the bacterial type II topoisomerase.

    Abstract translation: 本发明公开了一种新的喹苯偶氮自组装DNA和拓扑异构酶II-DNA复合物的复合物。 相关模型用于设计一系列可能具有抗癌活性或抗生素活性的喹喔啉恶唑，吡啶并苯并恶嗪，吡哆苯并吩ox嗪等相关化合物。 认为这些化合物的抗癌活性通过拓扑异构酶II-DNA复合物的稳定化和/或与G-四链体相互作用而起作用，而这些化合物的抗生素活性来源于它们抑制细菌II型拓扑异构酶促旋酶的能力。

    Ion triggered alkylation of biological targets by silyloxy aromatic agents
    18.
    发明授权
    Ion triggered alkylation of biological targets by silyloxy aromatic agents 失效
    离子触发由甲硅烷氧基芳香剂引发生物靶标的烷基化

    公开(公告)号：US5831073A

    公开(公告)日：1998-11-03

    申请号：US603221

    申请日：1996-02-20

    Applicant: Steven E. Rokita ,  Tianhu Li ,  Qingping Zeng

    Inventor： Steven E. Rokita ,  Tianhu Li ,  Qingping Zeng

    IPC: C07D207/404 ,  C07F7/18 ,  C07H19/04 ,  C07H21/00 ,  C07H23/00

    CPC classification number: C07F7/1852 ,  C07D207/404 ,  C07F7/1856 ,  C07H21/00 ,  C07H23/00

    Abstract: A silyloxy aromatic derivative capable of alkylating a target biological molecule when activated by ionic strength. A sequence directed reagent may be constructed by conjugating a methyl silyloxy aromatic derivative to a hexamethylamino linker attached to either the 5' or 3' terminus of an oligonucleotide. Annealing this modified fragment of DNA to its complementary sequence allows for target modification subsequent to ionic activation. The product of this reaction is a covalent crosslink between the reagent and target strands resulting from an alkylation of DNA by the activated silyloxy aromatic derivative. In a preferred embodiment, a nitrophenyl or bromo group is attached to a methyl group of the silyloxy aromatic derivative. This reagent may be similarly linked to an oligonucleotide probe. Activation of the alkylating agent by an ionic signal (X) which may naturally occur, or may be introduced into the media containing the target molecule, such as by the introduction of a salt (MX).

    Abstract translation: 当通过离子强度活化时，能够将靶生物分子烷基化的甲硅烷氧基芳族衍生物。 序列导向的试剂可以通过将甲基甲硅烷氧基芳族衍生物与连接到寡核苷酸的5'或3'末端的六甲基氨基接头共轭来构建。 将该修饰的DNA片段退火至其互补序列允许在离子活化后进行靶修饰。 该反应的产物是由活化的甲硅烷氧基芳族衍生物的DNA烷基化产生的试剂和靶链之间的共价交联。 在优选的实施方案中，硝基苯基或溴基连接到甲硅烷氧基芳族衍生物的甲基上。 该试剂可以类似地连接到寡核苷酸探针。 通过离子信号（X）活化烷基化剂，其可以天然存在，或者可以通过引入盐（MX）引入含有靶分子的介质中。

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