نتایج جستجو برای: isoindoline
تعداد نتایج: 246 فیلتر نتایج به سال:
A convenient, high yield conversion of doxorubicin to 3'-deamino-3'-(2''-pyrroline-1''-yl)doxorubicin is described. This daunosamine-modified analog of doxorubicin is 500-1000 times more active in vitro than doxorubicin. The conversion is effected by using a 30-fold excess of 4-iodobutyraldehyde in anhydrous dimethylformamide. The yield is higher than 85%. A homolog of this compound, 3'-deamino...
During the past five years ganglion-blocking agents have been used extensively in the treatment of arterial hypertension. The discovery of the activity of hexamethonium by Paton and Zaimis (1949) placed at our disposal an active therapeutic agent capable of producing a substantial reduction in the blood pressure. Subsequent research has been directed to the synthesis of new drugs offering advan...
Following the discovery of a new series of anti-acetylcholinesterase (anti-AChE) inhibitors such as 1-benzyl-4-[2-(N-benzoylamino)ethyl]piperidine (1), we reported that its rigid analogue, 1-benzyl-4-(2-isoindolin-2-ylethyl)piperidine (5), had more potent activity. We have extended the structure-activity relationship (SAR) study for the rigid analogue and found that the 2-isoindoline moiety in ...
A series of 3,5-bis(arylidene)-4-piperidone (DAP) compounds are considered as synthetic analogues of curcumin for anticancer properties. We performed structure-activity relationship studies by synthesizing a number of DAPs N-alkylated or acylated with nitroxides or their amine precursors as potent antioxidant moieties. Both subtituents on arylidene rings and on piperidone nitrogen (five- or six...
Pyruvate dehydrogenase kinase isoforms (PDKs 1-4) negatively regulate activity of the mitochondrial pyruvate dehydrogenase complex by reversible phosphorylation. PDK isoforms are up-regulated in obesity, diabetes, heart failure, and cancer and are potential therapeutic targets for these important human diseases. Here, we employed a structure-guided design to convert a known Hsp90 inhibitor to a...
A series of platinum(II) complexes with 1,3-bis(2-pyridylimino)isoindoline (BPI) derivatives were prepared by substitution of the coordinated Cl in the precursor complex Pt(BPI)Cl with a N-heterocyclic ligand such as pyridine, phthalazine or phenanthridine. These complexes display orange to red luminescence in fluid dichloromethane solutions and in the solid states at room temperature. The phot...
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