Synthesis, Activity, and Pharmacophore Development for Isatin-β-thiosemicarbazones with Selective Activity toward Multidrug-Resistant Cells
نویسندگان
چکیده
منابع مشابه
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.
We have recently identified a new class of compounds that selectively kill cells that express P-glycoprotein (P-gp, MDR1), the ATPase efflux pump that confers multidrug resistance on cancer cells. Several isatin-beta-thiosemicarbazones from our initial study have been validated and a range of analogues synthesized and tested. A number demonstrated improved MDR1-selective activity over the lead,...
متن کاملSynthesis and Antimicrobial Activity of Some New Isatin Derivatives
Some new 3-[(5-benzylidene-2-phenyl)-3, 5-dihydro-4-H-imidazol-4-one-3-(4-bezoylhydrazono)]-indole-2-ones (VIII) have been synthesized from different isatinhydrazones (II) by condensing with 2-phenyl-5-benzylidene- 3-N (4-acetyl phenyl)-1, 5-dihydro-imidazol-4-one (VII). Their chemical structures have been confirmed by IR, 1HNMR, MASS and by elemental analysis. Investigation of antimicrobial ac...
متن کاملSynthesis and Antimicrobial Activity of Some New Isatin Derivatives
Some new 3-[(5-benzylidene-2-phenyl)-3, 5-dihydro-4-H-imidazol-4-one-3-(4-bezoylhydrazono)]-indole-2-ones (VIII) have been synthesized from different isatinhydrazones (II) by condensing with 2-phenyl-5-benzylidene- 3-N (4-acetyl phenyl)-1, 5-dihydro-imidazol-4-one (VII). Their chemical structures have been confirmed by IR, 1HNMR, MASS and by elemental analysis. Investigation of antimicrobial ac...
متن کاملAntifungal Activity of Carvacrol on Ergosterol Synthesis in Multidrug Resistant Candida albicans
Introduction: Greatly increased use of antifungal therapies has resulted in the development of multidrug resistant. The phenolic compound carvacrol have been reported to have anti-Candida activity. This work is an attempt to examine effect of carvacrol on ergosterol synthesis against multidrug resistant Candida albicans. Methods: This cross-sectional study has been conducted on 30 immune-compr...
متن کاملSynthesis and Screening of Some New Isatin Containing Thiazole Derivatives for Antimicrobial Activity
In the present work, a series of new N’-[{5-(4-aryl) 1,3-thiazol-2yl}carbohydrazide-methyl]- 3(4-arylimino) indol-2-one analogs (5a-g) had heen synthesized from 3-(4-arylimino)-2-oxo- 1-indole-acetylthiosemicarbazide (4a-g) in ethanol, in the presence of phenacyl bromide or substituted phenacyl bromides. The compound 5e was characterized by its elemental analysis, IR, 1 HNMR and Mass Spectrosco...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2009
ISSN: 0022-2623,1520-4804
DOI: 10.1021/jm800861c