| abstract |
FIELD: pharmacology. n SUBSTANCE: invention relates to a new class of alkylating agents comprising a thienoindole fragment bound to a DNA-binding fragment of formula (I), (II) or (IV): n , and n n n n wherein R1 and R2 taken together form a group (D): n , n where R5 is a linear or branched C 1 -C 4 alkyl; R3 and R4 are hydrogen; R6 is halogen; T is absent or is N; BM means a DNA-binding fragment of formula (V): n , n where X is absent or is C 2 -C 4 alkenyl; Y is a group selected from n and n and Y' is a group selected from n and n and where R3 is hydrogen or a linear or branched C 1 -C 4 alkyl, and R15, R16 and R20 are independently hydrogen, hydroxy, NO 2 , C 1 -C 6 alkoxy substituted with C 5 -heterocyclyl containing nitrogen, -CONH-R3, where R3 is C 1 -C 6 alkyl substituted with aminocarbonyl, or -NR3R4, wherein R3 and R4 are hydrogen; U is a fragment of formula n or n where R3 is as defined above; Q is an integer from 0 to 4; L1 is hydrogen or L, where L is a fragment of the formula (Xj) cleavable under certain conditions: n , n where: R9 is hydrogen or C 1 -C 4 alkyl; W1 is absent; Z1 is absent, which exhibit cytotoxic activity and are useful for treatment of diseases such as cancer, cell proliferation disorders and viral infections. n EFFECT: increased efficiency of treatment. n 7 cl, 5 dwg, 7 ex |