Efficacious Cyclic N-Acyl O-Amino Phenol Duocarmycin Prodrugs
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چکیده
منابع مشابه
Asymmetric Synthesis of a CBI-Based Cyclic N-Acyl O-Amino Phenol Duocarmycin Prodrug
A short, asymmetric synthesis of a cyclic N-acyl O-amino phenol duocarmycin prodrug subject to reductive activation based on the simplified 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) DNA alkylation subunit is described. A key element of the approach entailed treatment of iodo-epoxide 7, prepared by N-alkylation of 6 with (S)-glycidal 3-nosylate, with EtMgBr at room temperature to ...
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Despite the prevalence of head-to-side chain threonine linkages in natural products, their incorporation has been underexplored in synthetic cyclic peptides. Herein we investigate a cyclic peptide scaffold able to undergo an N-O acyl rearrangement. Upon acylation of the amine with diverse carboxylic acids, the resulting cyclic depsipeptides displayed favorable cellular permeability and a confor...
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A simple, rapid and sensitive spectrophotometric method has been developed for the determination of Fe (II) by using N (o methoxy benzaldehyde) 2 aminophenol (NOMBAP) as an analytical reagent. NOMBAP has been synthesized and characterized by elemental and spectral analysis. NOMBAP extracts Fe (II) quantitatively (99.67%) into ethyl acetate from an aqueous solution of pH range 5.6 6.8. The ethyl...
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The title compound, C(13)H(11)N(3)O(3), is essentially planar (r.m.s. for the 19 non-H atoms = 0.031 Å), a conformation stabilized in part by intra-molecular O-H⋯N and N-H⋯O hydrogen bonds. The configuration about the imine bond [1.2919 (12) Å] is E. The presence of N-H⋯O(nitro) hydrogen bonds leads to the formation of supra-molecular tapes in the crystal structure. These are connected into lay...
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2013
ISSN: 0022-2623,1520-4804
DOI: 10.1021/jm400413r