256229-10-4Relevant articles and documents
Novel antimycin derivative containing 3-hydroxybenzoic acid group and preparation method and application thereof
-
Paragraph 0061-0064, (2020/06/20)
The invention relates to the technical field of medicinal chemistry, in particular to a novel-structure novel antimycin derivative containing 3-hydroxybenzoic acid group, produced by fermentation of streptomyces S.conglobates ATCC 31005, and a preparation method and application thereof in preparation of antitumor drugs. The molecular structure of the novel antimycin generally contains a 3-N-formylaminosalicylic acid group, while the molecular structure of the UAT-B-E provided by the invention is correspondingly provided with a 3-hydroxybenzoic acid group. An anti-tumor cell test finds that theinhibitory activity of UAT-B-E on human lung cancer cells, colorectal cancer cells and melanoma cells is equivalent to that of a control drug Cisplatin, and the toxicity to non-cancer cell lines is weak, so that UAT-B-E is expected to be developed into a tumor inhibitor.
Facially controlled C-methylation of oxolanyl and cyclopentyl acetate enolates: Application to the total synthesis of (+)-nephromopsinic acid
Mulzer, Johann,Steffen, Ulrich,Martin, Harry J.,Zorn, Ludwig
, p. 1028 - 1043 (2007/10/03)
The stereoselectivity of the C-methylation of oxolanyl and cyclopentyl acetate enolates 5a-22a was investigated. The configuration of the C-methyl diastereomers was elucidated by a combination of crystal structure analysis, NMR spectroscopy and chemical correlations. Generally, the methylation proceeded re*-selectively, although with very different degrees of selectivity. The most important stereodirecting effect was a steric one exerted by the 5-phenethyl substituent, and this steric effect was strongly increased by the stereodirecting effect of a 3-OR group. Contrary to previous literature evidence, the endocyclic oxolanyl oxygen does not exert an effect. These findings were applied in a highly stereoselective synthesis of (+)-nephromopsinic acid (94). Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005.