The present invention relates to tricyclic derivatives or pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. More precisely, the present invention relates to tricyclic derivatives as colchicine derivatives, pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. Tricyclic derivatives of the present invention show very powerful cytotoxicity to cancer cell lines but were much less toxic than colchicine or taxol, confirmed through animal toxicity test. Tricyclic derivatives of the invention also decrease the volume and weight of a tumor and have a strong angiogenesis inhibiting activity in HUVEC cells. Thus, tricyclic derivatives of the present invention can effectively be used as an anticancer agent, anti-proliferation agent and an angiogenesis inhibitor.
本发明涉及
三环衍
生物或其药学上可接受的盐、它们的制备方法以及含有它们的制药组合物。更具体地说,本发明涉及
三环衍
生物作为秋
水仙素衍
生物,药学上可接受的盐、它们的制备方法以及含有它们的制药组合物。本发明的
三环衍
生物对癌细胞株表现出非常强大的细胞毒性,但毒性比秋
水仙素或
紫杉醇要小得多,经动物毒性测试证实。本发明的
三环衍
生物还可以减少肿瘤的体积和重量,并在HU
VEC细胞中表现出强大的抑制血管生成的活性。因此,本发明的
三环衍
生物可以有效地用作抗癌剂、抗增殖剂和抑制血管生成剂。