(POLY) AMINOACETAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN, THEIR PROCESS OF PREPARATION AND THEIR APPLICATIONS IN THERAPEUTICS AS ANTICANCER AGENTS

摘要

Aminoacetamido epipodophyllotoxin derivatives (I) are new. Aminoacetamido epipodophyllotoxin derivatives of formula (I) and their salts are new: R 1, R 2H or Me; R3, A : H, 1-4C alkyl or benzyl, or A is (CH 2) aNR4B, or R3+A forms a 3-8C ring; a : 2-5; R4, B : H, 1-4C alkyl or benzyl, or B is (CH 2) bNR5(CH 2) cNR6R7 or (CH 2) cNR8R9, or R4+B forms a 3-8C ring; b, c : 2-5; R5-R7 : H, 1-4C alkyl or benzyl; R8, R9 : H or 1-5C alkyl, or together form a 3-8C ring or 4- to 8-membered heterocycle; R3+R4, R4+R5, R5+R6, R6+R7, R4+R8 : can also be 2-3C alkylene. An independent claim is also included for a process for preparing (I). [Image] ACTIVITY : Cytostatic. 2-(2-Dimethylaminoethylamino)-N-(9-(4-hydroxy-3,5-dimethoxyphenyl)-8-oxo-5,5a,6,8,8a,9-hexahydro-furo[3',4':6,7]naphtho[2,3-d][1,3]dioxol-5-yl)acetamide gave a 57% increase in survival time at a dose of 10 mg/kg in mice with P388 leukemia. MECHANISM OF ACTION : None given.