FIELD: chemistry.
SUBSTANCE: invention relates to compounds of formula (III) and formula (VI):
(III),
or pharmaceutically acceptable salts, cytotoxic dimers, conjugates of monomers and dimers thereof, where: double line
between N and C is a double bond, X is absent, and Y is H; W is C=O; R5 is OR, SH or NHR; optional R5 is a linking group or is selected from a polypyrrole, polyindolyl, polyimidazolyl, polypyrrole-imidazolyl, polypyrrole-indolyl or polyimidazole-indolyl link, optionally bearing a linking group; R6 is OR; R is H or linear or branched alkyl having from 1 to 3 carbon atoms; X' is CH2; Y' is O; and Z' is CH2; each A and A' is O; each D and D′ is linear alkyl having from 1 to 10 carbon atoms; L is absent or is a phenyl group, which is optionally substituted, where the substituent is a linking group that binds to the cell-binding agent through a covalent bond, or is selected from OR7, NR8R9 and OCOR11; R is H or linear or branched alkyl having from 1 to 3 carbon atoms; every R7, R8, R9, and R11 independently is H, linear or branched alkyl having from 1 to 10 carbon atoms, or a polyethylene glycol fragment -(OCH2CH2)n, where n is an integer from 1 to 10.
EFFECT: invention also relates to methods of using the compounds or conjugates for in vitro, in situ and in vivo diagnosis or treatment of mammalian cells or associated pathological conditions.
18 cl, 59 dwg, 7 tbl, 40 ex
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Authors
Dates
2019-03-28—Published
2010-02-04—Filed