BENZYLUREA DERIVATIVES AND COMPOSITION FOR ANTI-CANCER COMPRISING THE SAME, IN WHICH THE COMPOUNDS HAVE IMPROVED ANTI-CANCER ACTIVITY WITHOUT TOXICITY AND SIDE-EFFECTS, AND IMPROVED SOLUBILITY IN WATER

摘要

Purpose: the benzyl urea derived product and an ingredient for the identical compound of anti-human cancer are provided. Compound has improved anticancer activity nontoxicity and side effect, improves water-soluble. Construction: (4S) -1 benzyl -4- phenyl -2- imidazolidinone derivatives and pharmaceutically acceptable salt, hydrate and its solvent represented by formula (1) are provided, wherein Z1 is hydrogen or methyl; Z2 is hydrogen, hydroxyl, C1-C4 alkyl, C1-C4 alkyloxy, amino, C1-C4 alkylaminos or halogen; Z3 is hydrogen, halogen, C1-C4 alkyl, hydroxyl, C1-C4 alkyloxy, amino, nitro, containing cyanogen, R1R2N type amines, R3 (CH2) 1-4O type alkyloxy groups, selectively instead of a phenyl at least replacer, selected from hydroxyl, C1-C4 alkyloxy, amino, C1-C4 alkylaminos and nitro, or 5 or 6 circle heterocyclic ring base, it is by least one replacer, selected from amino, nitro, halogen, hydroxyl, containing cyanogen, C1-C4 alkyl, C1-C4 alkyloxy and C1-C4 alkylaminos selectively replace, including being selected from N, the non-homosexual of one or more of S and O; Z2 and Z3 forms a ring-O (CH2) 1-2O- ,-CH2CH2NR2 or CH=CH-CR4=CH- together; Z4 is hydrogen, C1-C4 alkyl, hydroxyl, C1-C4 alkyloxy, amino, C1-C4 alkylaminos or halogen; R1 is hydrogen or C1-C4 alkyl; R2 is hydrogen, C1-C4 alkyl, R3 (CH2) 1-4 types alkyl or COR5; R1 and R2 (CH2) 4-5 form a ring, and CO (CH2) 3-4, or (CH2) 2R6 (CH2) 2 form a ring together; R3 is phenyl, morpholine, thiomorpholine, N methyl piperazine, adjoins and cough up alkane, imidazol, N-(2- methoxyethyl)-N- methylamines, di (C1-C4 alkyl) amine, piperidines, the phenyl that nitro replaces or the phenyl of amino substitution; R4 is R3 (CH2) 2-4O type alkyloxy groups; R5 is C1-C4 alkyl, C1-C4 alkyloxy, C1-C4 alkylaminos, 2-thienylmethyl, selectively instead of a phenyl at least replacer, selected from hydroxyl, C1-C4 alkyloxy, amino, C1-C4 alkylaminos and nitro, or 5 or 6 circle heterocyclic ring base, it is by least one replacer, selected from amino, nitro, halogen, hydroxyl, containing cyanogen, C1-C4 alkyl, C1-C4 alkyloxy and C1-C4 alkylaminos selectively replace, including the non-homosexual of one or more selected from N, S and O; R6 is O, S or NR2.