Drug intelligence / Profile preview

C-1027 Aromatized chromophore

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
01

Overview

C-1027 Aromatized chromophore is the highly potent, active enediyne moiety of the macromolecular antitumor antibiotic C-1027. It is characterized by a nine-membered enediyne core that is responsible for its significant biological activity. Unlike some other enediynes, this molecule is inherently primed for cycloaromatization without external activation, leading to the formation of toxic 1,4-benzenoid diradical species. Its primary mechanism of action involves inducing oxygen-independent interstrand DNA crosslinks, as well as single- and double-stranded DNA breaks, which subsequently inhibit DNA synthesis and cause DNA damage. This unique oxygen-independent mechanism suggests its potential efficacy against hypoxic tumor cells. C-1027 Aromatized chromophore is considered one of the most potent cytotoxic molecules known due to its ability to induce a high ratio of DNA double-strand breaks. The larger C-1027 complex, of which this chromophore is the active component, has been investigated as an anticancer drug.

Other names
C-1027 chromophoreC1027 chromophoreC 1027 chromophoreLidamycin chromophoreC-1027 enediyne chromophoreC1027 enediyne chromophoreC 1027 enediyne chromophore
02

Targets

DNA

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