发明名称 |
DESIGN AND SYNTHESIS OF NOVEL TUBULIN POLYMERIZATION INHIBITORS: BONZOYLPHENYLURIA (BPU) SULFUR ANALOGS |
摘要 |
<p>A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC<SUB>50</SUB> of 2.1 µM.</p> |
申请公布号 |
WO2006113650(A1) |
申请公布日期 |
2006.10.26 |
申请号 |
WO2006US14449 |
申请日期 |
2006.04.18 |
申请人 |
JIMENO, ANTONIO;KHAN, SAEED, R.;HALLUR, GURULINGAPPA;HIDALAO, MANUEL |
发明人 |
KHAN, SAEED, R.;HALLUR, GURULINGAPPA;HIDALAO, MANUEL;JIMENO, ANTONIO |
分类号 |
A61K31/427;C07D239/38;A61K31/38;A61K31/404;A61K31/4152;A61K31/428;A61K31/505;A61P35/00;C07D209/04;C07D213/70;C07D237/18;C07D279/06;C07D279/08;C07D307/78 |
主分类号 |
A61K31/427 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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