| 摘要 |
PCT No. PCT/EP95/03823 Sec. 371 Date Mar. 21, 1997 Sec. 102(e) Date Mar. 21, 1997 PCT Filed Sep. 27, 1995 PCT Pub. No. WO96/11184 PCT Pub. Date Apr. 18, 1996The present invention relates to novel colchicine derivatives of formula (1), where Y is a -CH2-CH-NH-R3 group or a -CH-CH2OR3 group and the other variables are as defined in claim 1, having antiproliferative, antitumoral and anti-inflammatory activities. The novel compounds have a cytotoxicity on human tumoral cell lines comparable with colchicine, but, in comparison with the latter, they are less toxic and more selective, particularly on cells resistant to the usual medicaments. Some compounds have a marked activity on TNF and interleukine 2, and therefore are very potent anti-inflammatory agents. They can be included in pharmaceutical formulations useful for the parenteral, oral and topical administrations.
|
