echinomycin has been researched along with sandramycin* in 2 studies
1 review(s) available for echinomycin and sandramycin
Article | Year |
---|---|
Bisintercalator natural products with potential therapeutic applications: isolation, structure determination, synthetic and biological studies.
Echinomycin is the prototypical bisintercalator, a molecule that binds to DNA by inserting two planar chromophores between the base-pairs of duplex DNA, placing its cyclic depsipeptide backbone in the minor groove. As such, it has been the focus of an extensive number of investigations into its biological activity, nucleic acid binding and, to some extent, its structure-activity relationships. However, echinomycin is also the parent member of an extended family of natural products that interact with DNA by a similar mechanism of bisintercalation. The structural variety in these compounds leads to changes in sequence selectivity and and biological activity, particularly as anti-tumour and anti-viral agents. One of the more recently identified marine natural products that is moving close to clinical development is thiocoraline, and it therefore seems timely to review the various bisintercalator natural products. Topics: Biological Products; Depsipeptides; DNA; Echinomycin; Intercalating Agents; Peptides; Peptides, Cyclic; Quinolines; Quinoxalines | 2007 |
1 other study(ies) available for echinomycin and sandramycin
Article | Year |
---|---|
Synthesis and biological evaluation of quinaldopeptin.
The second-generation total synthesis of quinaldopeptin (1) was established via a Staudinger/aza-Wittig/diastereoselective Ugi three-component reaction sequence and a racemization-free [5 + 5] coupling and macrolactamization. A single-crystal X-ray structure of the chromophore analogue 26 confirmed the structural and stereochemical assignments of the macrocycle. Synthetic 1 successfully unwound supercoiled DNA to form a relaxed DNA in a dose-dependent manner, the binding affinity of 1 to four dsODNs was within a similar range (K(b) = 1.45-2.53 × 10(7) M(-1)), and the sequence selectivity was subtle. It was suggested that 1 possesses biological behaviors similar to those of sandramycin (2) in terms of cytotoxic activity against human cancer cell lines (IC50 = 3.2-12 nM) and HIF-1 inhibitory activity. Topics: Cell Line; Crystallography, X-Ray; DNA; Echinomycin; Humans; Hypoxia-Inducible Factor 1; Inhibitory Concentration 50; Molecular Structure; Peptides, Cyclic | 2014 |