NEW ALKYLATING AGENTS Russian patent published in 2017 - IPC C07D495/04 A61K31/407 A61P35/00 

FIELD: pharmacology.

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):

, and

wherein R1 and R2 taken together form a group (D):

,

where R5 is a linear or branched C₁-C₄ alkyl; R3 and R4 are hydrogen; R6 is halogen; T is absent or is N; BM means a DNA-binding fragment of formula (V):

,

where X is absent or is C₂-C₄alkenyl; Y is a group selected from

and

and Y' is a group selected from

and

and where R3 is hydrogen or a linear or branched C₁-C₄ alkyl, and R15, R16 and R20 are independently hydrogen, hydroxy, NO₂, C₁-C₆ alkoxy substituted with C₅-heterocyclyl containing nitrogen, -CONH-R3, where R3 is C₁-C₆ alkyl substituted with aminocarbonyl, or -NR3R4, wherein R3 and R4 are hydrogen; U is a fragment of formula

or

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:

,

where: R9 is hydrogen or C₁-C₄ 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.

EFFECT: increased efficiency of treatment.

7 cl, 5 dwg, 7 ex