The invention relates to 卤-oxygenated or 卤-thiolated carboxylic acid phenethylamide derivatives of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein A stands for optionally substituted aryl or optionally substituted heteroaryl; X is oxygen or sulfur; ...
4-Dimethylaminopyridine (DMAP) is a derivative of pyridine with the chemical formula (CH3)2NC5H4N. This colourless solid is of interest because it is more basic than pyridine, owing to the resonance stabilisation from the NMe2 substituent. Chemical Properties DMAP (m.p. 112-113°C) and PPY...
For example, targeting the poorly internalising antigen CD20 with an ADC consisting of the acid-labile 4-(4-acetylphenoxy)butanoic acid (AcBut) linker and the DNA minor groove-binding drug calicheamicin was effective in a preclinical lymphoma model, whereas substitution with an acid-stable (amide...
The racemic compound (ISAV-002), can be subjected to the desired enantiomerically pure compound (ISAV-003) by adding the appropriate chiral acid ((-)-CSA) (camphor sulfonic acid), then ISAV-003 is converted into the thioamide derivative (ISAV-004) by treatment with concentrated sulfuric ...
Herein, we show that the tetrahydroisoquinoline 1H-indole-2-carboxylic acid {4-[2-(cyano-3,4-dihydro-1H-isoquinolin-2-yl)-ethyl]-cyclohexyl}-amide (SB269,652) behaves as an atypical, allosteric antagonist at D(3) and D(2) receptors. Accordingly, SB269,652 potently (low nanomolar range...
(Fig.3d, upper panel). A synthetic flavone derivative AhR antagonist, alpha-naphthoflavone (ANF)34, inhibited BaP-induced PD-L1 at both mRNA (Fig.3e) and protein (Fig.3d, lower panel) levels. Since ANF also bears agonistic effect on AhR in that it can activate AhR targetCYP1A1promoter...
General Description 4-Dimethylaminopyridine (DMAP) is a derivative of pyridine with the chemical formula (CH3)2NC5H4N. This colourless solid is of in..
aSynthesis of Z-338 (EN:262475): Z-338 can be prepared by two closely related ways: 1) Acylation of 2-aminothiazole-4-carboxylic acid ethyl ester (I) with 2,4,5-trimethoxybenzoyl chloride (II) gives the corresponding amide (III). The 2-methoxy group of (III) is then selectively cle...
The carboxy groups of these sugars would be linked to the N-terminus of the peptide via an amide linkage. Presently, the preferred N-terminal modification is a methoxy-succinyl modification. Cell-secreted peptidases which recognize particular amino acid sequences are also well known to ordinarily ...
However, when the dienes are intermediates for the synthesis of steroids having the C/D-trans-orientation, this technique of using the free carbonyl derivative is not particularly desirable. When monoenes of formula I-b having C/D-trans configuration are desired, it is preferable to first ...