申请人:——
公开号:US20040266747A1
公开(公告)日:2004-12-30
Novel tumour selective anti-neoplastic agents are characterized, in that to customary antineoplastic agents are attached one or two very specific unbranched &OHgr;-hydroxyalkyl, (&OHgr;-hydroxy)alkenyl, &OHgr;-(2,3-dihydroxypropyloxy)alkyl or an (&OHgr;-(2,3-dihydroxypropyloxy))alkenyl groups R
2
and R
3
with 5 to 30 carbon atoms, forming a tumour selective conjugate as exemplified with the compounds of formulae I, II and III [] wherein R
1
is a customary pharmaceutically acceptable inorganic or organic leaving group and A is 1,2-dimethylene, 1,3-trim ethylene, 1,2-cyclopentylene or 1,2-cyclohexylene. These compounds as well as their pharmaceutically acceptable salts, ester and prodrug derivatives are valuable chemotherapeutics
1
新型肿瘤选择性抗肿瘤药物的特点是将常规抗肿瘤药物与一个或两个非常特定的无支链&OHgr;-羟基烷基、(&OHgr;-羟基)烯基、&OHgr;-(2,3-二羟基丙氧基)烷基或一个(&OHgr;-(2,3-二羟基丙氧基))烯基的基团R2和R3连接起来,形成一个肿瘤选择性结合物,例如化合物I、II和III的式子[]其中R1是常规的医药上可接受的无机或有机离去基团,A是1,2-二甲基、1,3-三甲基、1,2-环戊基或1,2-环己基。这些化合物及其医药上可接受的盐、酯和前药衍生物是有价值的化疗药物。