239477-77-1Relevant academic research and scientific papers
3-SUBSTITUTED PIPERIDINE-2, 6-DIONES AND NON-COVALENT COMPLEXES WITH ALBUMIN
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Page/Page column 44, (2016/06/06)
The present disclosure provides derivatives of 3-substituted piperidine-2, 6-diones, non-covalently bound complexes with serum albumin, pharmaceutical compositions of the same, and methods of use thereof. The non-covalently bound complexes are significant
Novel Analogs of Camptothecin
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Paragraph 0342; 0343; 0344; 0359, (2014/05/20)
The present invention provides novel conjugates of camptothecin and camptothecin analogs with a linker and an HSA-binding moiety. The novel conjugates are prodrug forms of the camptothecin or camptothecin analogs and can be used to treat mammalian cell pr
SOLUBLE COMPLEXES OF DRUG ANALOGS AND ALBUMIN
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Page/Page column 45-46, (2014/08/19)
The present invention provides novel, non-covalently bound complexes of serum albumin and analogs of poorly soluble drugs, such as camptothecin. The novel complexes are significantly more water-soluble than the camptothecin analogs and are useful as prodr
Structure-function studies on nucleoside antibiotic mureidomycin A: Synthesis of 5′-functionalised uridine models
Gentle, Caragh A.,Harrison, Stephen A.,Inukai, Masatoshi,Bugg, Timothy D. H.
, p. 1287 - 1294 (2007/10/03)
The importance of functional groups in nucleoside antibiotic mureidomycin A (MRD A) for biological activity has been examined by derivatisation of samples of the natural product, and by synthesis of uridine-containing analogues. N-Succinyl and di- and tri-acetyl derivatives MRD A have been prepared, and were found to have reduced activity as inhibitors of E. coli translocase I. The enamide alkene of MRD A was found to be extremely resistant towards hydrogenation by a variety of reagents. Several 5′-functionalised uridine derivatives were synthesised from N3-p-methoxybenzyl-2′,3′-isopropylideneuridine. A series of 5′-aminoacyl derivatives were prepared, and the 3-aminopropionyl (IC50 260 μM) and 7-aminoheptanoyl (IC50 1.5 mM) derivatives were found to act as reversible inhibitors. An analogue mimicking the carboxy terminus of MRD A was synthesised, and also acted as an inhibitor of translocase I (IC50 1.9 mM). A phosphonate analogue designed as a possible suicide inhibitor showed modest inhibition (IC50 3.7 mM), which was shown to be irreversible.
