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1.发明授权NOVEL CATIONIC 17 ALPHA- SUBSTITUTED-ESTRADIOL DERIVATIVES USEFUL AS ANTI-CANCER AGENT 有权新型阳离子17α被取代的雌二醇为手段对抗癌症
公开(公告)号：EP2111409B1
公开(公告)日：2012-06-27
申请号：EP07859632.7
申请日：2007-12-31
IPC分类号： C07J41/00 , A61K31/565 , A61P35/00
CPC分类号： C07J41/0044
摘要： The present invention provides a novel series of cationic, lipid-based, 17α-substituted-estradiol derivatives. The present invention further provides a process for the preparation of a novel series of 17α-substituted-estradiol derivatives. The invention also provides information about highly selective anticancer activities of these molecules in estrogen responsive cell lines. The compound elicits high level of toxicity to gynecological cancer cell lines such as MCF-7, T47D (estrogen receptor positive cell lines), MDA-MB-468 (estrogen receptor knock-out cell line), HeIa (cervical cancer). The present class of cationic lipid-based, estradiol derivatives is likely to find specific use in developing target specifically deliverable anticancer drugs for the treatment of gynecological cancers that are most prevalent in women population irrespective of ethnicity.
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2.发明公开NOVEL CATIONIC 17 ALPHA- SUBSTITUTED-ESTRADIOL DERIVATIVES USEFUL AS ANTI-CANCER AGENT 有权新型阳离子17α被取代的雌二醇为手段对抗癌症
公开(公告)号：EP2111409A1
公开(公告)日：2009-10-28
申请号：EP07859632.7
申请日：2007-12-31
IPC分类号： C07J41/00 , A61K31/565 , A61P35/00
CPC分类号： C07J41/0044
摘要： The present invention provides a novel series of cationic, lipid-based, 17α-substituted-estradiol derivatives. The present invention further provides a process for the preparation of a novel series of 17α-substituted-estradiol derivatives. The invention also provides information about highly selective anticancer activities of these molecules in estrogen responsive cell lines. The compound elicits high level of toxicity to gynecological cancer cell lines such as MCF-7, T47D (estrogen receptor positive cell lines), MDA-MB-468 (estrogen receptor knock-out cell line), HeIa (cervical cancer). The present class of cationic lipid-based, estradiol derivatives is likely to find specific use in developing target specifically deliverable anticancer drugs for the treatment of gynecological cancers that are most prevalent in women population irrespective of ethnicity.
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