Design, synthesis, and anti-breast cancer evaluation of new triarylethylene analogs bearing short alkyl- and polar amino-/amido-ethyl chains.

The synthesis of novel triarylethylene analogs, designed based on well-known Selective Estrogen Receptor Modulators (SERMs), i.e., ospemifene and tamoxifen, as potential anti-breast cancer agents is described.

Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents.

The synthesis of some novel Ospemifene derived analogs and their evaluation as anti-breast cancer agents against MCF-7 (ER-positive) and MDA-MB-231 (ER-negative) human breast cancer cell lines are described. Few of these analogs for instance, compounds 6, 7 and 8 are shown to be more effective than recent Selective Estrogen Receptor Modulators (SERMs) i.e.

Synthesis, docking and in vitro antimalarial evaluation of bifunctional hybrids derived from β-lactams and 7-chloroquinoline using click chemistry.

1,2,3-Triazole tethered β-lactam and 7-chloroquinoline bifunctional hybrids were synthesized and evaluated as potential antimalarial agents. Activity against cultured Plasmodium falciparum was dependent on the N-substituent of the β-lactam ring as well as the presence of bis-triazole at the C-3 position. The observed activity profiles were further substantiated by docking studies via inhibition of P.

1,2,3-Triazole tethered β-lactam-chalcone bifunctional hybrids: synthesis and anticancer evaluation.

The manuscript describes the synthesis of novel 1,2,3-triazole tethered β-lactam-chalcone bifunctional hybrids via click chemistry approach utilizing azide-alkyne cycloaddition reactions and their evaluation as anticancer agents against four human cancer cell lines. The presence of a cyclohexyl substituent at N-1 of β-lactam ring and methoxy substituents, preferably ortho on ring A and para on ring B on chalcones markedly improved the anticancer profiles of the synthesized scaffolds with the most potent of the test compound exhibiting an IC(50) value of <1, 67.1, <1 and 6.

Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives.

3-Azido-, 3-amino- and 3-(1,2,3-triazol-1-yl)-β-lactams were synthesized and evaluated for their antiplasmodial activity against four strains of Plasmodium falciparum and KB cells for their cytotoxicity profiles. The presence of a cyclohexyl substituent at N-1 and a phenyl group on the triazole ring markedly improved the activity profiles of triazole-tethered β-lactam exhibiting IC(50) values of 1.13, 1.

Highly selective potentiometric determination of mercury(II) ions using 1-furan-2-yl-4-(4-nitrophenyl)-2-phenyl-5H-imidazole-3-oxide based membrane electrodes.

The electrode characteristics and selectivities of PVC-based mercury(II) selective coated graphite electrode (CGE) and polymeric membrane electrode (PME) incorporating the recently synthesized 1-furan-2-yl-4-(4-nitrophenyl)-2-phenyl-5H-imidazole-3-oxide are reported here. The electrodes exhibit Nernstian slope for mercury(II) ions over wide concentration ranges, i.e.

PASS-assisted exploration of antidepressant activity of 1,3,4-trisubstituted-beta-lactam derivatives.

Assisted by PASS predictions, the antidepressant activity of 1,3,4-trisubstituted monocyclic beta-lactams in seasonal affective disorders is described.

PASS-predicted design, synthesis and biological evaluation of cyclic nitrones as nootropics.

Out of 400 virtually designed imidazoline N-oxides, five cyclic nitrones were selected on the basis of PASS prediction as potent nootropics and were evaluated for their biological activities in albino mice. The selected N-alkyl and aryl-substituted nitrones were found to be excellent nootropics. A series of lead compounds acting as cognition enhancers have been provided, which can be further exploited in search of such New Chemical Entities (NCEs).

PASS assisted search and evaluation of some azetidin-2-ones as C.N.S. active agents.

Purpose: The present study evaluates some azetidin-2-ones derivatives for their central nervous system (CNS) modulating activities. The compounds were chosen from a series (5a-o) which were previously synthesized and evaluated for hypolipidemic and antihyperglycemic activity based on the predictions made by the computer software "Prediction of Activity Spectra for Substances (PASS)".

Material And Methods: The test compounds were predicted to have a variety of biological activities but those with the best potential for CNS modulating activity were selected for evaluation of a particular CNS activity as 5a for anti-anxiety, 5b, 5n and 5j for nootropic activity and compound 5c anti-catatonic and anti-dyskinetic activities.

2,6-bis-methylsulfanyl-[1,3,5]thiadiazine-4-thione as a Ag+-selective ionophore.

A silver ion-selective electrode was prepared with a polymeric membrane incorporating 2,6-bis-methylsulfanyl-[1,3,5]thiadiazine-4-thione as an ionophore, tri-n-butylphosphate (TBP) as a plasticizer and sodium tetraphenylborate (NaTPB) as an additive. The electrode exhibited a near-Nernstian response of 52 mV/decade over a wide linear concentration range of 1.0 x 10(-5) - 1.

Synthesis and biological activity of novel antibacterial quinazolines.

Novel quinazolines, having interesting antibacterial activity have been prepared, characterized and tested against a panel of susceptible and resistant Gram positive and Gram negative organisms.

Amidine derived 1,3-diazabuta-1,3-dienes as potential antibacterial and antifungal agents.

Several 1-aryl-2-phenyl-4-piperidino-4-thioalkyl-1,3-diazabuta-1,3-dienes were prepared by the treatment of N-arylimino isothiocyanate with piperidine followed by S-alkylation with alkyl iodides in the presence of dry acetone and potassium hydroxide. The constitution of the products was supported by IR, PMR and mass spectral study. The compounds synthesized were tested in in vitro against E.

Evaluation of anti-hyperglycemic activity of some novel monocyclic beta lactams.

Purpose: The present study was undertaken to examine the effect of monocyclic beta-lactams (compounds 5a-5o) for anti-hyperglycemic activity against alloxan-induced diabetes in rats. As these compounds have been shown to control disturbances in cholesterol metabolism induced by diabetes.

Methods: The test compounds were synthesized via [2+2] cycloaddition (Staudinger) reaction of imines with ketenes.

Synthesis and antibacterial evaluation of 4-substituted-2-phenyl-1-p-tolyl-4-thiomethyl-1,3-diazabuta-1,3-dienes: a novel class of antibacterial agents.

A series of novel-2-phenyl-1-p-tolyl-4-thiomethyl-1,3-diazabuta-1,3-dienes compounds (5a-5e) possessing morpholino, diethyl amino, pyrrolidino, piperidino and 2-aminopyridino groups respectively at C-4 were prepared by reaction of alpha-aryliminobenzyl isothiocyanates with secondary amines and S-alklyation of the resultant thioureas with aqueous potassium hydroxide. The isothiocyanates were obtained from easily available starting materials. These 1,3-diazabuta-1,3-dienes were obtained in pure form after recrystallization and their structures were established by analytical and spectral data.