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SG2285, a novel C2-aryl-substituted pyrrolobenzodiazepine dimer prodrug that cross-links DNA and exerts highly potent antitumor activity.
TLDR
SG2285 is defined as a highly active cytotoxic compound with antitumor properties desirable for further development and shown in several human tumor xenograft models, including ovarian, non-small cell lung, prostate, pancreatic, and melanoma, with cures obtained in the latter model with a single dose.
DNA interstrand cross-linking and in vivo antitumor activity of the extended pyrrolo[2,1-c][1,4]benzodiazepine dimer SG2057
TLDR
SG2057 is therefore a highly active antitumor agent, with more potent in vitro activity and superior in vivo activity to SG2000, warranting further development.
Linker length modulates DNA cross-linking reactivity and cytotoxic potency of C8/C8' ether-linked C2-exo-unsaturated pyrrolo[2,1-c][1,4]benzodiazepine (PBD) dimers.
TLDR
The C2-exo-unsaturated PBD dimers 4a,b are not only more effective than their C-ring saturated counterparts in terms of induced DeltaTm shift, but they also exert this effect more rapidly.
SG2285, a novel C2-aryl-substituted pyrrolobenzodiazepine dimer prodrug with potent antitumor activity
TLDR
A modification of the single cell gel electrophoresis (comet) assay has shown SG2285 to be highly efficient at producing ICLs in cells, which form more slowly than those produced by SG2202.
Molecular and cellular pharmacology of novel pyrrolo [2,1-c] [1,4] diazepine-based anticancer agents
TLDR
Q2lQT-exo-unsaturated PBD dimers have been characterised to be highly cytotoxic and efficient in producing interstrand crosslinks both in naked DNA and in cells that are not repaired up to 48 hours.
Poster Session 1 — Medicinal Chemistry
TLDR
Early findings show that energies appear superior for the NMR rather than the crystal structure using one selected quinoxaline-functionalised AAQ ligand, and that the available binding sites differ markedly in affinity for ligand.
Cancer esearch apeutics , Targets , and Chemical Biology 285 , a Novel C 2-Aryl-Substituted Pyrrolobenzodiazepine er Prodrug That Cross-links DNA and Exerts Highly R ent Antitumor Activity
TLDR
SG2285 was defined as a highly active cytotoxic compound with antitumor properties desirable for further development and showed activity in several human xenograft models, including ovarian, non–small cell lung, prostate, pancreatic, and melanoma.