发明名称 |
Synthesis of 8H-3A-aza-cyclopenta [A ]indenes and 5,10-dihydropyrrolo[1,2-B]isoquinolines derivatives and their use as antitumor therapeutic agents |
摘要 |
The present disclosure relates to a series of bis(hydroxymethyl) and its bis(carbamate) of 8H-3a-azacyclopenta[a]indene-1-yl and 5,10-dihydropyrrolo-[1,2-b]isoquinolines derivatives (Formula I-Formula IV) as DNA di-alkylating agents. The preliminary antitumor studies indicated that compounds disclosed herein could exhibit potent cytotoxicity in vitro and antitumor therapeutic efficacy in human tumor xenografts and could have little or no cross-resistance to either Taxol or Vinblastine. The results demonstrated that compounds disclosed herein possess potent antitumor therapeutic efficacy and are expected to have potential for clinical applications. |
申请公布号 |
US8410130(B2) |
申请公布日期 |
2013.04.02 |
申请号 |
US20080267227 |
申请日期 |
2008.11.07 |
申请人 |
SU TSANN-LONG;CHOU TING-CHAO;ACADEMIA SINICA |
发明人 |
SU TSANN-LONG;CHOU TING-CHAO |
分类号 |
A61K31/437;A61K31/403;C07D221/06;C07D487/00 |
主分类号 |
A61K31/437 |
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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