126092-97-5Relevant articles and documents
Synthesis of a mitomycin C-lexitropsin hybrid
Champeil, élise,Sapse, Anne-Marie
, p. 1190 - 1196 (2014)
We have constructed hybrid drugs where mitomycin C is linked to the N-methylpyrrole carboxamide framework present in lexitropsins. The coupling reactions leading to these products are efficient and the yields are very high. An interesting spectroscopic feature of these hybrids is the red shift observed in the UV-vis spectrum. Although DFT calculations indicate the possible existence of complexes formed during the coupling reactions, these complexes were not detected. The only species produced and isolated were the mitomycin C-mono- and bis-N-methyl pyrrole conjugates.
PBD ANTIBACTERIAL AGENTS
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Page/Page column 84; 85, (2017/07/18)
The invention relates to pyrrolobenzodiazepines compounds (PBDs) and to pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular, to treat bacterial infections. The PBDs are compounds of formula (I): and salts and solvates thereof; wherein: dotted lines indicates the optional presence of a double bond; X, X1, X2, X3 and X4 are connecting functional groups; L is C1-12 alkylene; R4, R5 and R6 are independently selected from phenylene, cyclopentanylene, cyclohexanylene, 5 - to 9 -membered heteroarylene and 5 - to 6-membered hetereocyclylene groups, and these groups are optionally substituted with up to three optional substituent groups; R7 is selected from N(C1-6 alkyl)(C1-6alkyl), 5 - to 6-membered nitrogen-containing hetereocyclyl groups, a monosaccharide moiety and an amino monosaccharide moiety wherein these groups are optionally substituted; and R8 and R9 either together form a double bond, or are selected from H and OR14, or R8 is a prodrug moiety and R9 is OR14; m is 0 or 1; with the proviso that when X4 is C(O)NH then the up to three optional substituents of R7 are not selected from (CH2)k -CO2R12; with the proviso that when X4 is (CH2)tO then R4 is not phenylene, m is 1 and R6 is not a 5 - to 9 -membered heteroarylene; and with the proviso that when X4 is C(O)NH or NHC(O) that R4 and/or R6 is not 5 - to 9 -membered heteroarylene.
CONJUGATES FOR TREATING DISEASES
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Page/Page column 126, (2016/10/04)
The present disclosure relates to pyrrolobenzodiazepine (PBD) prodrugs and conjugates thereof. The present disclosure also relates to pharmaceutical compositions of the conjugates described herein, methods of making and methods of using the same.
