The first total syntheses of izenamides A, B, and C, which are depsipeptides inhibitor of cathepsin D, were accomplished. In addition, the stereochemistry of izenamide B was confirmed by our syntheses.
Changjin Lim
doaj +1 more source
A New Depsipeptide Antibiotic, Variapeptin [PDF]
A culture similar to Streptomyces variabilis was found to produce a novel cyclic hexadepsipeptide antibiotic named variapeptin. Variapeptin is structurally related to azinothricin, A83586C, and citropeptin. The antibiotic was active against Gram-positive bacteria and showed cytotoxic activity against mammalian cells.
NAKAGAWA, Masaya +3 more
openaire +3 more sources
On-resin multicomponent 1,3-dipolar cycloaddition of cyclopentanone–proline enamines and sulfonylazides as an efficient tool for the synthesis of amidino depsipeptide mimics [PDF]
Depsipeptides are biologically active peptide derivatives that possess a high therapeutic interest. The development of depsipeptide mimics characterized by a chemical diversity could lead to compounds with enhanced features and activity. In this work, an
Pieraccini, Stefano +7 more
core +1 more source
Biosynthetic Modularity Rules in the Bisintercalator Family of Antitumor Compounds
Diverse actinomycetes produce a family of structurally and biosynthetically related non-ribosomal peptide compounds which belong to the chromodepsipeptide family. These compounds act as bisintercalators into the DNA helix.
Javier Fernández +7 more
doaj +1 more source
Chemical Classification of Cyclic Depsipeptides
Cyclic depsipeptides (CDPs) are a family of cyclic peptide-related compounds, of which the ring is mainly composed of amino- and hydroxy acid residues joined by amide and ester bonds (at least one), leading to a wide diversity of fascinating chemical structures. They differ in both their ring structure and their side chains, especially by the nature of
Taevernier, Lien +3 more
openaire +3 more sources
Bouillonamide: A Mixed Polyketide–Peptide Cytotoxin from the Marine Cyanobacterium Moorea bouillonii
The tropical marine cyanobacterium, Moorea bouillonii, has gained recent attention as a rich source of bioactive natural products. Continued chemical investigation of this cyanobacterium, collected from New Britain, Papua New Guinea, yielded a novel ...
Lik Tong Tan +2 more
doaj +1 more source
Depsipeptide inhibits removal of incorporated 5-aza-CdR from DNA.
(A) H719 cells were incubated with [3H]-5-aza-CdR for 48 hrs, with presence or absence of depsipeptide at 0.1 µM for the first 6 hrs (depsipeptide+[3H]-5-aza-CdR) or last 6 hrs ([3H]-5-aza-CdR+depsipeptide) and then washed with cold PBS.
Donglai Wang (49052) +15 more
core +1 more source
Total synthesis and biological evaluation of fluorinated cryptophycins
Cryptophycins are cytotoxic natural products that exhibit considerable activities even against multi-drug-resistant tumor cell lines. As fluorinated pharmaceuticals have become more and more important during the past decades, fluorine-functionalized ...
Christine Weiß +3 more
doaj +1 more source
The HDAC inhibitor depsipeptide transactivates the p53/p21 pathway by inducing DNA damage
Histone deacetylase (HDAC) inhibitors have been proven to be effective therapeutic agents to kill cancer cells through inhibiting HDAC activity or altering the structure of chromatin.
Bo Tu +13 more
core +1 more source
Enhancement of depsipeptide-mediated apoptosis of lung or esophageal cancer cells by flavopiridol: Activation of the mitochondria-dependent death-signaling pathway [PDF]
Objective: Treating cancer cells with depsipeptide, a novel antitumor agent currently in a phase II clinical trial, causes potent upregulation of p21/WAF1 expression and cell arrest at G1 and G2 checkpoints.
Steiner, Federico +11 more
core +1 more source

