Browsing by Subject "drug synthesis"

Article

1,2,3-Dithiazoles-new reversible melanin synthesis inhibitors: A chemical genomics study

Charalambous, Anna; Koyioni, Maria; Antoniades, Ioanna; Pegeioti, Despoina; Eleftheriou, Iro; Michaelidou, Sophia S.; Amelichev, Stanislav A.; Konstantinova, L. S.; Rakitin, O. A.; Koutentis, Panayiotis Andreas; Skourides, Paris A. (2015)

A chemical genomic screen of an in-house library of small molecule heterocycles was carried out using Xenopus laevis embryos. This led to the identification of N-(4-chloro-5H-1,2,3-dithiazol-5-ylidene)-4-methoxyaniline ...

Article

Cancer chemopreventive activity of brassinin, a phytoalexin from cabbage

Mehta, R. G.; Liu, J.; Constantinou, Andreas I.; Thomas, C. F.; Hawthorne, M.; You, M.; Gerhäuser, C.; Pezzuto, J. M.; Moon, R. C.; Moriarty, R. M. (1995)

Brassinin [3-(S-methyldithiocarbamoyl aminomethyl indole], a phytoalexin first identified as a constituent of cabbage, was synthesized and evaluated for cancer chemopreventive activity. Dose-dependent inhibition of ...

Article

The conversion of isothiazoles into pyrazoles using hydrazine

Ioannidou, Heraklidia A.; Koutentis, Panayiotis Andreas (2009)

The conversion of isothiazoles into pyrazoles on treatment with hydrazine is investigated. The influence of various C-3, C-4 and C-5 isothiazole substituents and some limitations of this ring transformation are examined. ...

Article

Design, synthesis and biological evaluation of benzo[e][1,2,4]triazin-7(1H) -one and [1,2,4]-triazino[5,6,1-jk]carbazol-6-one derivatives as dual inhibitors of beta-amyloid aggregation and acetyl/butyryl cholinesterase

Catto, M.; Berezin, Andrey A.; Lo Re, D.; Loizou, G.; Demetriades, Marina; De Stradis, A.; Campagna, F.; Koutentis, Panayiotis Andreas; Carotti, A. (2012)

Alzheimer's disease (AD) onset and progression are associated with the dysregulation of multiple and complex physiological processes and a successful therapeutic approach should therefore address more than one target. Two ...

Article

Discovery of anti-cancer activity for benzo[1,2,4]triazin-7-ones: Very strong correlation to pleurotin and thioredoxin reductase inhibition

Sweeney, M.; Coyle, R.; Kavanagh, P.; Berezin, Andrey A.; Lo Re, D.; Zissimou, Georgia A.; Koutentis, Panayiotis Andreas; Carty, Michael P.; Aldabbagh, Fawaz (2016)

The thioredoxin (Trx)–thioredoxin reductase (TrxR) system plays a key role in maintaining the cellular redox balance with Trx being over-expressed in a number of cancers. Inhibition of TrxR is an important strategy for ...

Article

Fabrication, characterization, and evaluation in drug release properties of magnetoactive poly(ethylene oxide)-poly(l -lactide) electrospun membranes

Savva, I.; Odysseos, A. D.; Evaggelou, L.; Marinica, O.; Vasile, E.; Vekas, L.; Sarigiannis, Y.; Krasia-Christoforou, T. (2013)

The fabrication of electrospun magnetoactive fibrous nanocomposite membranes based on the water-soluble and biocompatible poly(ethylene oxide) (PEO), the biocompatible and biodegradable poly(l-lactide) (PLLA) and preformed ...

Article

Multistage nanoparticles for improved delivery into tumor tissue

Stylianopoulos, T.; Wong, C.; Bawendi, M. G.; Jain, R. K.; Fukumura, D. (2012)

The enhanced permeability and retention (EPR) effect has been a key rationale for the development of nanoscale carriers to solid tumors. As a consequence of EPR, nanotherapeutics are expected to improve drug and detection ...

Article

Novel lipophilic amidate oxorhenium and oxotechnetium complexes as potential brain agents: Synthesis, characterization and biological evaluation

Papadopoulos, Minas S.; Nock, B.; Maina-Nock, Theodosia; Pirmettis, Ioannis C.; Raptopoulou, Catherine P.; Tasiopoulos, Anastasios J.; Troganis, Anastassios N.; Kabanos, Themistoklis A.; Terzis, Aris; Chiotellis, Efstratios (2001)

Novel oxorhenium and oxotechnetium complexes based on the tetradentate 1-(2-hydroxybenzamido)-2-(pyridinecarboxamido)benzene, H3L, ligand have been synthesized and characterized herein. Thus, by reacting equimolar quantities ...

Article

A quorum sensing regulated small volatile molecule reduces acute virulence and promotes chronic infection phenotypes

Kesarwani, M.; Hazan, R.; He, J.; Que, Y.; Apidianakis, Yiorgos; Lesic, B.; Xiao, G.; Dekimpe, V.; Milot, S.; Déziel, Eric; Lépine, F.; Rahme, L. G. (2011)

A significant number of environmental microorganisms can cause serious, even fatal, acute and chronic infections in humans. The severity and outcome of each type of infection depends on the expression of specific bacterial ...

Article

Reinvestigating the synthesis of N-arylbenzamidines from benzonitriles and anilines in the presence of AlCl3

Koutentis, Panayiotis Andreas; Mirallai, Styliana I. (2010)

The preparation of N-phenylbenzamidine 3a from the reaction between benzonitrile Ia and aniline in the presence of AId3 is reinvestigated with respect to mode of reagent addition, reaction temperature and Lewis acid ...

Article

Ring transformations of 2-hydroxy-(4-chloro-5H-1,2,3-dithiazol-5-ylideneamino)arenes

Kalogirou, Andreas S.; Michaelidou, Sophia S.; Koyioni, Maria G.; Koutentis, Panayiotis Andreas (2015)

Abstract The cyclisation reactions of 2-(4-chloro-5H-1,2,3-dithiazol-5-ylidene-amino)phenol (5a), 3-(4-chloro-5H-1,2,3-dithiazol-5-ylideneamino)pyridin-2-ol (5b) and 2-(4-chloro-5H-1,2,3-dithiazol-5-ylideneamino)pyridin-3-ol ...

Article

Structure based inhibitor design targeting glycogen phosphorylase b. Virtual screening, synthesis, biochemical and biological assessment of novel N-acyl-β-d-glucopyranosylamines

Parmenopoulou, Vanessa; Kantsadi, Anastassia L.; Tsirkone, Vicky G.; Chatzileontiadou, Demetra S. M.; Manta, Stella; Zographos, Spyros E.; Molfeta, Christina; Archontis, Georgios Z.; Agius, Loranne; Hayes, Joseph M.; Leonidas, Demetres D.; Komiotis, Dimitris (2014)

Glycogen phosphorylase (GP) is a validated target for the development of new type 2 diabetes treatments. Exploiting the Zinc docking database, we report the in silico screening of 1888 N-acyl-β-d-glucopyranosylamines ...

Article

Structure-activity relationships of brassinin in preventing the development of carcinogen-induced mammary lesions in organ culture

Mehta, R. G.; Liu, J.; Constantinou, Andreas I.; Hawthorne, M.; Pezzuto, J. M.; Moon, R. C.; Moriarty, R. M. (1994)

Brassinin, a pkytoalexin, is found in Chinese cabbage. Previously, we showed that brassinin significantly inhibited dimethylbenz(a)anthracene (DMBA)-induced mammary lesions in organ culture. Moreover, it was an effective ...

Article

Synthesis and study of the cancer cell growth inhibitory properties of α-, γ-tocopheryl and γ-tocotrienyl 2-phenylselenyl succinates

Vraka, Panayiota S.; Drouza, Chryssoula; Rikkou, Maria P.; Odysseos, Andreani D.; Keramidas, Anastasios D. (2006)

Vitamin E succinate selenium-conjugated molecules were synthesized and their apoptogenic properties were evaluated. 4-Methyl-2-phenylselenyl succinate (4) was prepared by the reaction of sodium benzeneselenolate with ...

Article

Synthesis of fused 1,2,4-dithiazines and 1,2,3,5-trithiazepines

Koyioni, Maria G.; Manoli, Maria; Koutentis, Panayiotis Andreas (2014)

Reacting ( Z)-N-(4-chloro-5H-1,2,3-dithiazol-5-ylidene)-1H-pyrazol-5-amines 5 with Et2NH and then with concd H2SO4 gives 5H-pyrazolo[3,4-e ][1,2,4]dithiazine-3-carbonitriles 7 in good yields (74-85%) and 6H-pyrazolo-[3,4 ...

Article

The synthesis of pyrrolo[2,3-c][1,2,6]thiadiazine-5-carbonitriles from (4H-1,2,6-thiadiazin-4-ylidene)malononitriles

Kalogirou, Andreas S.; Koutentis, Panayiotis Andreas; Rikkou-Kalourkoti, Maria D. (2010)

[3,5-Bis(dialkylamino)-4H-1,2,6-thiadiazin-4-ylidene]propanedinitriles 6a-c, react with sodium methoxide or ethoxide to give the corresponding 6-alkoxy-4-dialkylamino substituted pyrrolo[2,3-c][1,2,6]thiadiazine-5-carbonitriles ...

Article

Synthesis of sulfur containing analogues of the soluble guanylate cyclase inhibitor 8-bromo-4H-[1,2,4]oxadiazolo[3,4-c][1,4]benzoxazin-1-one NS2028

Berezin, Andrey A.; Koutentis, Panayiotis Andreas; Manos, Manolis J. (2011)

Sulfur analogues of the soluble guanylate cyclase (sGC) inhibitor NS2028 1a are synthesized. Treating 8-bromo-2H-benzo[b][1,4]oxazin-3(4H)-one oxime (6) with 1,1′-thiocarbonyldiimidazole (1.1 equiv) gave the carbamothioate ...

Article

Synthesis, characterization and biological studies of new antimony(III) halide complexes with ω-thiocaprolactam

Ozturk, I. I.; Banti, Christina N.; Manos, Manolis J.; Tasiopoulos, Anastasios J.; Kourkoumelis, Nikolaos; Charalabopoulos, Konstantinos A.; Hadjikakou, Sotiris K. (2012)

Three new antimony(III) halide complexes (SbX 3, X = Cl, Br and I) with the heterocyclic thione ω-thiocaprolactam (1-azacycloheptane-2- thione, (Hthcl)) of formulae {[SbCl 2(μ 2-Cl)(Hthcl) 2] n} (1), {[(SbBr 2(μ 2-Br)(Hthcl) ...

Article

Synthesis, structure, and biological activity of a new insulinomimetic peroxovanadium compound: Bisperoxovanadium imidazole monoanion [3]

Crans, D. C.; Keramidas, Anastasios D.; Hoover-Litty, H.; Anderson, O. P.; Miller, M. M.; Lemoine, L. M.; Pleasic-Williams, S.; Vandenberg, M.; Rossomando, A. J.; Sweet, L. J. (1997)

Article

A theoretical study of chlorine atom and methyl radical addition to nitrogen bases: Why do Cl atoms form two-center - Three electron bonds whereas CH3 radicals form two-center - Two-electron bonds?

McKee, M. L.; Nicolaïdes, Andrew N.; Radom, L. (1996)

Ab initio molecular orbital calculations have been carried out on a series of adducts between chlorine atom and NH3, NMe3, NCl3, HN=CH2, and pyridine, and between methyl radical and HN=CH2 and pyridine. A two-center-three-electron ...