- Structure-activity relationships of monomeric C2-aryl pyrrolo[2,1- c ][1,4]benzodiazepine (PBD) antitumor agents
-
A comprehensive SAR investigation of the C2-position of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) monomer antitumor agents is reported, establishing the molecular requirements for optimal in vitro cytotoxicity and DNA-binding affinity. Both carbocyclic and
- Antonow, Dyeison,Kaliszczak, MacIej,Kang, Gyoung-Dong,Coffils, Marissa,Tiberghien, Arnaud C.,Cooper, Nectaroula,Barata, Teresa,Heidelberger, Sibylle,James, Colin H.,Zloh, Mire,Jenkins, Terence C.,Reszka, Anthony P.,Neidle, Stephen,Guichard, Sylvie M.,Jodrell, Duncan I.,Hartley, John A.,Howard, Philip W.,Thurston, David E.
-
supporting information; experimental part
p. 2927 - 2941
(2010/09/14)
-
- Synthesis and DNA binding affinity of novel A-C8/C-C2-exo unsaturated alkoxyamido-linked pyrrolo[2,1-c][1,4]benzodiazepine dimers.
-
The synthesis of novel A-C8/C-C2-exo unsaturated alkoxyamido-linked pyrrolo[2,1-c][1,4]benzodiazepine dimers is reported and these dimers show significant DNA binding affinity and they also exhibit moderate anticancer activity.
- Kamal, Ahmed,Srinivas,Ramulu,Ramesh,Kumar, P Praveen,Kumar, M Shiva
-
p. 4337 - 4350
(2007/10/03)
-
- PYRROLOBENZODIAZEPINES
-
Compounds of formula (I) : formula (I) and salts, solvates, chemically protected forms, and prodrugs thereof, are disclosed wherein R2 is selected from: an optionally substituted napthyl group; an optionally substituted thiophenyl or furanyl gr
- -
-
-
- 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.
- -
-
Page 40, 106
(2010/11/29)
-
- 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.
- Cooper, Nectaroula,Hagan, David R.,Tiberghien, Arnaud,Ademefun, Temitope,Matthews, Charles S.,Howard, Philip W.,Thurston, David E.
-
p. 1764 - 1765
(2007/10/03)
-