发明名称 |
CONJUGATES OF NITROIMIDAZOLES AND THEIR USE AS CHEMOTHERAPEUTIC AGENTS |
摘要 |
Novel compounds which are derivatives of tetra-O-methyl nordihydroguaiaretic acid (NDGA), as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof are provided. These NDGA derivatives have a nitroimidazole moiety and these derivatives show preferential toxicity to hypoxic cells as hypoxic cytotoxins. Their cytotoxicity toward hypoxic cells is a result of abstraction of hydrogen from target molecules by free radicals formed in the reduction of the nitro group. This makes the disclosed compounds an effective anti cancer drug because hypoxic cells are generally considered to be more resistant to anti cancer drugs than normal cells. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including hepatocellular carcinoma, breast cancer and prostate cancer, are also provided. |
申请公布号 |
WO2012166778(A2) |
申请公布日期 |
2012.12.06 |
申请号 |
WO2012US39959 |
申请日期 |
2012.05.30 |
申请人 |
THE JOHNS HOPKINS UNIVERSITY;NATIONAL TSING HUA UNIVERSITY;HUANG, RU CHIH C.;MOLD, DAVID EDWARD;HWU, JIH RU;HSU, MING HUA;WU, SZU CHUN |
发明人 |
HUANG, RU CHIH C.;MOLD, DAVID EDWARD;HWU, JIH RU;HSU, MING HUA;WU, SZU CHUN |
分类号 |
C07D233/60;A61K31/4164;A61P35/00 |
主分类号 |
C07D233/60 |
代理机构 |
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代理人 |
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地址 |
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