abstract |
Uracil derivatives represented by general formula (1) or salts thereof, wherein R1 represents chloro, bromo, iodo, cyano or lower alkyl; and R2 represents a 4- to 8-membered heterocycle optionally substituted by lower alkyl, imino, hydroxy, hydroxymethyl, methanesulfonyloxy, amino or nitro and having one to three nitrogen atoms, amidinothio wherein hydrogen on nitrogen is optionally substituted by lower alkyl, guanidino wherein hydrogen on nitrogen is optionally substituted by lower alkyl or cyano, lower alkylamidino, amino wherein hydrogen on nitrogen is optionally substituted by lower alkyl, -CH¿2?N(R?a)Rb¿ (wherein R?a and Rb¿ are the same or different and each represents hydrogen or lower alkyl, or R?a and Rb¿ together with the nitrogen atom to which they are bonded may form pyrrolidine), -NH-(CH¿2?)m-Z (wherein Z represents amino wherein hydrogen on nitrogen is optionally substituted by lower alkyl, or cyano; and m is an integer of 0 to 3), -NR?c(CH¿2)m-OH (wherein Rc represents hydrogen or lower alkyl; and n is a natural number of 1 to 4), -X-Y (wherein X represents S or NH; and Y represents 2-imidazolin-2-yl, 2-imidazolyl, 1-methylimidazol-2-yl, 1,2,4-triasol-3-yl, 2-pyrimidyl or 2-benzimidazolyl optionally substituted by lower alkyl), or ureido or thioureido wherein hydrogen on nitrogen is optionally substituted by lower alkyl; and drugs containing the same, such as antitumor effect potentiators and antitumor agents. |