71904-80-8Relevant articles and documents
First total synthesis of aerucyclamide B
Pe?a, Stella,Scarone, Laura,Manta, Eduardo,Serra, Gloria
, p. 2806 - 2808 (2013)
The first total synthesis of the antimalarial aerucyclamide B has been achieved in 9% overall yield. Two thiazoles and a dipeptide were used to prepare two open precursors of cyclo-Gly-l-allo-Thr-l-Ile-Thz-d-allo-Ile-Thz. Cyclodehydration with Deoxo-Fluor of the β-hydroxyamide present in the macrocycle, rendered aerucyclamide B (67%) and an unexpected fluorous derivative (28%).
Analog of dolastatin 3. Synthesis, 1H NMR studies and spatial conformation
Bernier,Houssin,Henichart
, p. 2695 - 2702 (1986)
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Synthesis of a Microcystis aeruginosa predicted metabolite with antimalarial activity
Pena, Stella,Scarone, Laura,Manta, Eduardo,Stewart, Lindsay,Yardley, Vanessa,Croft, Simon,Serra, Gloria
, p. 4994 - 4997 (2012)
The synthesis of a Microcystis aeruginosa predicted metabolite analog of aerucyclamide B was performed. This hexacyclopeptide was obtained from three heterocyclic building blocks by a convergent macrocycle-assembly methodology. The compound exhibited good in vitro antiplasmodial activity (IC50: 0.18 μM, K1, cholorquine resistant strain).
Total Synthesis of the Post-translationally Modified Polyazole Peptide Antibiotic Goadsporin
Dexter, Hannah L.,Williams, Huw E. L.,Lewis, William,Moody, Christopher J.
supporting information, p. 3069 - 3073 (2017/03/13)
The structurally unique polyazole antibiotic goadsporin contains six heteroaromatic oxazole and thiazole rings integrated into a linear array of amino acids that also contains two dehydroalanine residues. An efficient total synthesis of goadsporin is repo
Discovery of Novel Class i Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities
Yao, Yiwu,Tu, Zhengchao,Liao, Chenzhong,Wang, Zhen,Li, Shang,Yao, Hequan,Li, Zheng,Jiang, Sheng
supporting information, p. 7672 - 7680 (2015/10/20)
A successful structure-based design of novel cyclic depsipeptides that selectively target class I HDAC isoforms is described. Compound 11 has an IC50 of 2.78 nM for binding to the HDAC1 protein, and the prodrugs 12 and 13 also exhibit promising antiproliferative activities in the nanomolar range against various cancer cell lines. Compounds 12 and 13 show more than 20-fold selectivity toward human cancer cells over human normal cells in comparison with romidepsin (FK228), demonstrating low probability of toxic side effects. In addition, compound 13 exhibits excellent in vivo anticancer activities in a human prostate carcinoma (Du145) xenograft model with no observed toxicity. Thus, prodrug 13 has therapeutic potential as a new class of anticancer agent for further clinical translation.