260418-10-8

Upstream product

• 260418-07-3 trifluoromethanesulphonic acid (11aS)-1,11a-dihydro-5,11-dioxo-10-(2-trimethylsilanylethoxymethyl)-7,8-dimethoxy-5H-pyrrolo[2,1-c][1,4]benzodiazepine-2-yl ester 
• 98-80-6 phenylboronic acid 
• 4998-07-6 4,5-dimethoxy-2-nitro-benzoic acid 
• 260418-04-0 (11aS)-1,2,3,11a-tetrahydro-10-(2-trimethylsilanylethoxymethyl)-7,8-dimethoxy-2-(tert-butyl-dimethylsilanyloxy)-5H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11-dione 
• 260418-05-1 (11aS)-1,2,3,11a-tetrahydro-10-(2-trimethylsilanylethoxymethyl)-7,8-dimethoxy-2-hydroxy-5H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11-dione 
• 260418-06-2 (11aS)-1,11a-dihydro-(2-trimethylsilanylethoxymethyl)-7,8-dimethoxy-5H-pyrrolo[2,1-c][1,4]benzodiazepine-2,5,11-trione 
• 260418-03-9 2-(tert-butyl-dimethyl-silanyloxy)-7,8-dimethoxy-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11-dione 
• 54431-30-0 1-(4,5-dimethoxy-2-nitrobenzoyl)-4-hydroxypyrrolidine-2-carboxylic acid methyl ester 
• 260418-02-8 (2R,11aS)-2-hydroxy-7,8-dimethoxy-1,2,3,10,11,11a-hexahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11-dione 

Relevant academic research and scientific papers

Synthesis of novel C2-aryl pyrrolobenzodiazepines (PBDs) as potential antitumour agents

Three novel C2-aryl substituted pyrrolobenzodiazepines (PBDs) have been synthesised and evaluated in a number of cell lines revealing selective cytotoxicity at the sub-nanomolar level towards melanoma and ovarian cancer cell lines.

Pyrrolobenzodiazepines

Compounds of the formulae Ia and Ib: wherein: A is CH2, or a single bond; R2 is selected from: R, OH, OR, CO2H, CO2R, COH, COR, SO2R, CN; R6, R7 and R9 are independently selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn; and R8 is selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn, where R is as defined above, or the compound is a dimer with each monomer being the same or different and being of formula Ia or Ib, where the R8 groups of the monomers form together a bridge having the formula —X—R′—X— linking the monomers, where R′ is an alkylene chain containing from 3 to 12 carbon atoms, which chain may be interrupted by one or more hetero-atoms and/or aromatic rings and may contain one or more carbon-carbon double or triple bonds, and each X is independently selected from O, S, or N; except that in a compound of formula Ia when A is a single bond, then R2 is not CH═CH(CONH2) or CH═CH(CONMe2). Other related compounds are also disclosed.

Pyrrolobenzodiazepines

Compounds of the formulae Ia and Ib: wherein:A is CH2, or a single bond;R2 is selected from: R, OH, OR, CO2H, CO2R, COH, COR, SO2R, CN;R6, R7 and R9 are independently selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn;and R8 is selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn, where R is as defined above, or the compound is a dimer with each monomer being the same or different and being of formula Ia or Ib, where the R8 groups of the monomers form together a bridge having the formula -X-R'-X- linking the monomers, where R' is an alkylene chain containing from 3 to 12 carbon atoms, which chain may be interrupted by one or more hetero-atoms and/or aromatic rings and may contain one or more carbon-carbon double or triple bonds, and each X is independently selected from O, S, or N; except that in a compound of formula Ia when A is a single bond, then R2 is not CH=CH(CONH2) or CH=CH(CONMe2). Other related compounds are also disclosed.