| 摘要 |
Described herein are novel 1-aryl-3-(2-chloroethyl)ureas derivatives. These derivatives are useful anticancer agents having excellent specify towards ce ll targets and potent antineoplastic activity without systemic toxicity or mutagenicity. More specifically, the invention is directed to novel derivatives of formula (I), wherein R1 is C1-C6 lower alkyl, C3-C7 cycloalky l, C1-C6 lower alkoxy, C1-C6 hydroxy alkyl, or C1-C6 lower halide; R2 is H, C1- C6 lower alkyl, C3-C7 cycloalkyl, C1-C6 lower alkoxy, C1-C6 hydroxy alkyl or C1 - C6 lower halide, di-halide or tri-halide; R1 and R2 may also be part of cycl ic structures expressed by formula (II), R3 and R4 are as defined in R5 or, halide, di-halide, trihalide, C1-C7 lower dialkyl, or alicyclic groups of structure (III), wherein n = 2 to 8 carbon atoms, said alicyclic ring can be substituted by one or more groups as defined in R5; or polycyclic rings bearing not more than three rings wherein the rings other than the ring bearing the substituted 2-chloroethylamino moiety can be substituted by one or more groups as defined in R5; R5 is H, C1-C7 lower alkyl, C1-C7 lower alkoxy , C1-C7 hydroxy alkyl, C1-C7 amino alkyl, C1-C6 thio alkyl, C1-C5 S-lower alky l, C1-C7 N-lower alkyl, C1-C7 N,N-dilower alkyl, C1-C7 lower cyanoalkyl, C1-C7 lower haloalkyl, C1-C7 lower sulfoxide or C3-C7 cycloalkyl; or a prodrug thereof. Also disclosed are pharmaceutical compositions containing the compounds of the invention in conjunction with a pharmaceutically acceptable carrier and the use of the compositions in treating cancer.
|
