Search results for: Jadwiga Handzlik

Items from 1 to 20 out of 31 results

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Pharmacophoric features for a very potent 5‐spirofluorenehydantoin inhibitor of cancer efflux pump ABCB1, based on X‐ray analysis

Ewa Żesławska, Annamária Kincses, Gabriella Spengler, Wojciech Nitek, more

Chemical Biology & Drug Design > 93 > 5 > 844 - 853

In order to extend knowledge about pharmacophoric features responsible for ABCB1 inhibitory properties of imidazolidin‐2,4‐dione derivatives, 1′‐[4‐(4‐(o‐methoxyphenyl)‐piperazin‐1‐yl)butyl]‐3′‐methyl‐spiro(fluoren‐9,5′‐imidazolidine)‐2′,4′‐dione (3) and its salt (4) with rhodanine‐3‐acetic acid (RA) were prepared and investigated by X‐ray diffraction method, as well as their efflux modulating effects...

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The Anticancer and Chemopreventive Activity of Selenocyanate-Containing Compounds

Wesam Ali, Mónica Álvarez-Pérez, Małgorzata Anna Marć, Noemi Salardón-Jiménez, more

Current Pharmacology Reports > 2018 > 4 > 6 > 468-481

Purpose of the Review The aim of this work is to review systematically the selenocyanate-containing compounds reported so far with potential applications in cancer prevention and in cancer treatment, attempting to focus on the most active selenocyanate derivatives. Recent Findings The chemopreventive and anticancer activity of selenocyanate-containing compounds as p-xylene selenocyanate and benzyl...

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In the search for a lead structure among series of potent and selective hydantoin 5‐HT₇R agents: The drug‐likeness in vitro study

Gniewomir Latacz, Annamaria Lubelska, Magdalena Jastrzębska‐Więsek, Anna Partyka, more

Chemical Biology & Drug Design > 90 > 6 > 1295 - 1306

Since the year 1993, when 5‐HT₇ receptor (5‐HT₇R) was discovered, there is no selective 5‐HT₇R ligand introduced to the pharmaceutical market. One out of the main reasons disqualifying the 5‐HT₇R ligands is weak drugability properties, including metabolic instability or low permeability. This study is focused on the search of a lead compound by “drug‐likeness” estimation of the first series of selective...

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Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H3 receptor ligands

Dorota Łażewska, Maria Kaleta, J. Stephan Schwed, Tadeusz Karcz, more

Bioorganic & Medicinal Chemistry > 2017 > 25 > 20 > 5341-5354

Novel biphenyloxy-alkyl derivatives of piperidine and azepane were synthesized and evaluated for their binding properties at the human histamine H₃ receptor. Two series of compounds were obtained with a meta- and a para-biphenyl moiety. The alkyl chain spacer contained five and six carbon atoms. The highest affinity among all compounds was shown by 1-(6-(3-phenylphenoxy)hexyl)azepane (13) with a K...

article

Spectroscopic investigations of novel pharmaceuticals: Stability and resonant interaction with laser beam

Adriana Smarandache, Mihai Boni, Ionut Relu Andrei, Jadwiga Handzlik, more

Applied Surface Science > 2017 > 417 > C > 143-148

This paper presents data about photophysics of two novel thio-hydantoins that exhibit promising pharmaceutical properties in multidrug resistance control. Time stability studies are necessary to establish the proper use of these compounds in different applications. As for their administration as drugs, it is imperative to know their shelf life, as well as storage conditions.At the same time, laser...

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The computer-aided discovery of novel family of the 5-HT6 serotonin receptor ligands among derivatives of 4-benzyl-1,3,5-triazine

Dorota Łażewska, Rafał Kurczab, Małgorzata Więcek, Katarzyna Kamińska, more

European Journal of Medicinal Chemistry > 2017 > 135 > C > 117-124

The work describes a discovery of new chemical family of potent ligands for the 5-HT₆ serotonin receptors. During the search for new histamine H₄ receptor antagonists among 1,3,5-triazine derivatives, compound 2 (4-benzyl-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine) was found. Compound 2, weakly active for the H₄ receptor but fitted in 3/4 of pharmacophore features of the 5-HT₆R ligand, occurred...

article

Natural selenium particles from Staphylococcus carnosus: Hazards or particles with particular promise?

Ethiene Castellucci Estevam, Sharoon Griffin, Muhammad Jawad Nasim, Polina Denezhkin, more

Journal of Hazardous Materials > 2017 > 324 > PA > 22-30

Various bacteria, including diverse Staphylococci, reduce selenite to yield red selenium particles with diameters in the high nanometer to low micrometer range. Formation and accumulation of such particles in bacteria often results in cell death, triggered by a loss of thiols and formation of disruptive deposits inside the cell. Hence certain pathogenic bacteria are rather sensitive to the presence...

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Selenoesters and selenoanhydrides as novel multidrug resistance reversing agents: A confirmation study in a colon cancer MDR cell line

Márió Gajdács, Gabriella Spengler, Carmen Sanmartín, Małgorzata Anna Marć, more

Bioorganic & Medicinal Chemistry Letters > 2017 > 27 > 4 > 797-802

Taking into account that multidrug resistance (MDR) is the main cause for chemotherapeutic failure in cancer treatment and as a continuation of our efforts to overcome this problem we report the evaluation of one cyclic selenoanhydride (1) and ten selenoesters (2–11) in MDR human colon adenocarcinoma Colo 320 cell line. The most potent derivatives (1, 9–11) inhibited the ABCB1 efflux pump much stronger...

article

Laser beam resonant interaction of new hydantoin derivatives droplets for possible biomedical applications

Adriana Smarandache, Viorel Nastasa, Mihai Boni, Angela Staicu, more

Colloids and Surfaces A: Physicochemical and Engineering Aspects > 2016 > 505 > C > 37-46

This paper deals with the rapid molecular changes induced by laser radiation on two novel hydantoin derivatives, generically named SZ-2 and SZ-7, having promising pharmaceutical properties as Szymanska et al. in 2002 and Subtelna et al. in 2010 have reported. Hydantoins solutions with concentration of 10⁻³M in dimethyl sulfoxide were exposed both in droplets and bulk samples to coherent radiation...

article

Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors

Ewa Szymańska, Anna Drabczyńska, Tadeusz Karcz, Christa E. Müller, more

Bioorganic & Medicinal Chemistry > 2016 > 24 > 18 > 4347-4362

A new series of 32 pyrimido- and 5 tetrahydropyrazino[2,1-f]purinediones was obtained and evaluated for their adenosine receptors (ARs) affinities. The 1,3-dibutyl derivative of 9-(4-(2-(dimethylamino)ethoxy)phenyl)-6,7,8,9-tetrahydropyrimido[1,2-f]purine-2,4(1H,3H)-dione was found to be the most potent A₁ AR antagonist of the present series, showing selectivity over the other AR subtypes. The structure–activity...

article

The 5-aromatic hydantoin-3-acetate derivatives as inhibitors of the tumour multidrug resistance efflux pump P-glycoprotein (ABCB1): Synthesis, crystallographic and biological studies

Ewa Żesławska, Annamária Kincses, Gabriella Spengler, Wojciech Nitek, more

Bioorganic & Medicinal Chemistry > 2016 > 24 > 12 > 2815-2822

A series of arylpiperazine derivatives of hydantoin-3-acetate, including previously obtained 5,5-diphenylhydantoin (1–7) and new-synthesized spirofluorene-hydantoin derivatives (8–12), were investigated in the search for new inhibitors of the tumour multidrug resistance (MDR) efflux pump P-glycoprotein (P-gp, ABCB1) overexpressed in mouse T-lymphoma cells. Synthesis of new compounds (8–12) was performed...

article

Identification of selenocompounds with promising properties to reverse cancer multidrug resistance

Enrique Domínguez-Álvarez, Márió Gajdács, Gabriella Spengler, Juan Antonio Palop, more

Bioorganic & Medicinal Chemistry Letters > 2016 > 26 > 12 > 2821-2824

In previous studies, 56 novel selenoesters and one cyclic selenoanhydride with chemopreventive, antiproliferative and cytotoxic activity were described. Herein, the selenoanhydride and selected selenoesters were evaluated for their ability to reverse the cancer multidrug resistance (MDR) using the ABCB1 efflux pump inhibition assay in mouse MDR T-lymphoma cells. Results showed that the selenoanhydride...

article

Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation

Katarzyna Kucwaj-Brysz, Dawid Warszycki, Sabina Podlewska, Jagna Witek, more

European Journal of Medicinal Chemistry > 2016 > 112 > C > 258-269

A series of novel arylpiperazine 5-(4-fluorophenyl)-5-methylhydantoins with 2-hydroxypropyl linker (2–15) was synthesized and evaluated on their affinity towards serotonin 5-HT₇ receptor (5-HT₇R) in comparison to other closely related GPCRs: serotonin 5-HT_1A, and dopamine D₂ receptors. The functional activity studied through the measurement of 5-HT₇R-mediated cyclic AMP production in Human Embryonic...

article

Imidazolidine-4-one derivatives in the search for novel chemosensitizers of Staphylococcus aureus MRSA: Synthesis, biological evaluation and molecular modeling studies

Anna Matys, Sabina Podlewska, Karolina Witek, Jagna Witek, more

European Journal of Medicinal Chemistry > 2015 > 101 > C > 313-325

A series of amine derivatives of 5-aromatic imidazolidine-4-ones (7–19), representing three subgroups: piperazine derivatives of 5-arylideneimidazolones (7–13), piperazine derivatives of 5-arylideneimidazolidine-2,4-dione (14–16) and primary amines of 5-naphthyl-5-methylimidazolidine-2,4-diones (17–19), was evaluated for their ability to improve antibiotics effectiveness in two strains of Gram-positive...

article

SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT7 receptor ligands among phenylpiperazine hydantoin derivatives

Jadwiga Handzlik, Andrzej J. Bojarski, Grzegorz Satała, Monika Kubacka, more

European Journal of Medicinal Chemistry > 2014 > 78 > C > 324-339

The current study is focused on newly developed phenylpiperazine derivatives of aromatic methylhydantoin differing in mutual positions of methyl and phenyl moieties. The new compounds were synthesized using Bucherer–Bergs reaction, two-phase alkylation, Mitsunobu reaction and/or an alkylation under microwave irradiation. The compounds developed were assessed on their affinity for serotoninergic receptors...

article

Temperature dependence of the interaction of prazosin with lipid Langmuir monolayers

Barbara Gzyl-Malcher, Jadwiga Handzlik, Ewelina Klekowska

Colloids and Surfaces B: Biointerfaces > 2013 > 112 > Complete > 171-176

The influence of temperature on membrane–prazosin interactions was studied. Prazosin, a quinazoline derivative of 2-furoylpiperazine, is a classic antihypertensive and antiarrhythmic drug. A mixed cholesterol/phospholipid monolayer at the water/air interface was employed as a simplified biomembrane model. Brewster angle microscopy (BAM) was used to visualize the monolayer morphology. It was found...

article

Synthesis, biological activity and molecular modelling studies of tricyclic alkylimidazo-, pyrimido- and diazepinopurinediones

Anna Drabczyńska, Tadeusz Karcz, Ewa Szymańska, Meryem Köse, more

Purinergic Signalling > 2013 > 9 > 3 > 395-414

Syntheses and biological activities of imidazo-, pyrimido- and diazepino[2,1-f]purinediones containing N-alkyl substituents (with straight, branched or unsaturated chains) are described. Tricyclic derivatives were synthesized by the cyclization of 8-bromo-substituted 7-(2-bromoethyl)-, 7-(3-chloropropyl)- or 7-(4-bromobutyl)-theophylline with primary amines under various conditions. Compound 22 with...

article

Search for new tools to combat Gram-negative resistant bacteria among amine derivatives of 5-arylidenehydantoin

Jadwiga Handzlik, Ewa Szymańska, Sandrine Alibert, Jacqueline Chevalier, more

Bioorganic & Medicinal Chemistry > 2013 > 21 > 1 > 135-145

A series of amine-alkyl derivatives of 5-arylidenehydantoin 3–21 was evaluated for their ability to improve antibiotic effectiveness in two strains of Gram-negative Enterobacter aerogenes: the reference strain (ATCC-13048) and the chloramphenicol-resistant derivative over-producing the AcrAB-TolC efflux pump (CM-64). Three antibiotics, chloramphenicol, nalidixic acid and sparfloxacin were used as...

article

Interaction of prazosin with model membranes — A Langmuir monolayer study

Barbara Gzyl-Malcher, Jadwiga Handzlik, Ewelina Klekowska

Bioelectrochemistry > 2012 > 87 > Complete > 96-103

In this study, the effect of prazosin on the molecular interactions between cholesterol and 1,2-dipalmitoylphosphatidylcholine (DPPC) within a monolayer at an air–water interface was studied. A mixed cholesterol/DPPC monolayer was employed as a model lipid membrane.From a detailed analysis of surface pressure–area isotherms, it was concluded that DPPC and cholesterol were miscible and formed non-ideal...

article

Synthesis and SAR-study for novel arylpiperazine derivatives of 5-arylidenehydantoin with α1-adrenoceptor antagonistic properties

Jadwiga Handzlik, Ewa Szymańska, Renata Wójcik, Anna Dela, more

Bioorganic & Medicinal Chemistry > 2012 > 20 > 14 > 4245-4257

The study is focused on a series of 5-arylidenehydantoin derivatives with a phenylpiperazine-hydroxypropyl fragment at N3 of the hydantoin ring. The compounds were assessed on their affinity for α ₁ -adrenoceptors and evaluated in functional bioassays for their antagonistic properties. Crystal structures of (Z)-5-(4-chlorobenzylidene)-3-(3-(4-(2-ethoxyphenyl)piperazin-1-yl)-2-hydroxypropyl)imidazolidine-2,4-dione...

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Search results for: Jadwiga Handzlik

Pharmacophoric features for a very potent 5‐spirofluorenehydantoin inhibitor of cancer efflux pump ABCB1, based on X‐ray analysis

The Anticancer and Chemopreventive Activity of Selenocyanate-Containing Compounds

In the search for a lead structure among series of potent and selective hydantoin 5‐HT₇R agents: The drug‐likeness in vitro study

Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H3 receptor ligands

Spectroscopic investigations of novel pharmaceuticals: Stability and resonant interaction with laser beam

The computer-aided discovery of novel family of the 5-HT6 serotonin receptor ligands among derivatives of 4-benzyl-1,3,5-triazine

Natural selenium particles from Staphylococcus carnosus: Hazards or particles with particular promise?

Selenoesters and selenoanhydrides as novel multidrug resistance reversing agents: A confirmation study in a colon cancer MDR cell line

Laser beam resonant interaction of new hydantoin derivatives droplets for possible biomedical applications

Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors

The 5-aromatic hydantoin-3-acetate derivatives as inhibitors of the tumour multidrug resistance efflux pump P-glycoprotein (ABCB1): Synthesis, crystallographic and biological studies

Identification of selenocompounds with promising properties to reverse cancer multidrug resistance

Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation

Imidazolidine-4-one derivatives in the search for novel chemosensitizers of Staphylococcus aureus MRSA: Synthesis, biological evaluation and molecular modeling studies

SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT7 receptor ligands among phenylpiperazine hydantoin derivatives

Temperature dependence of the interaction of prazosin with lipid Langmuir monolayers

Synthesis, biological activity and molecular modelling studies of tricyclic alkylimidazo-, pyrimido- and diazepinopurinediones

Search for new tools to combat Gram-negative resistant bacteria among amine derivatives of 5-arylidenehydantoin

Interaction of prazosin with model membranes — A Langmuir monolayer study

Synthesis and SAR-study for novel arylpiperazine derivatives of 5-arylidenehydantoin with α1-adrenoceptor antagonistic properties

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