Synthesis and biological evaluation of new bischromone derivatives with antiproliferative activity.

abstract：:Synthesis of 2-chloro-1,1-dimethylethyl and 2-chloro-2,2-dimethylethyl analogues of ifosfamide was performed via aziridine intermediate. In vitro metabolic activation showed that both compounds are metabolised at a rate similar to the parent drug. However, their anticancer activity against L1210 leukaemia in mice was ...

journal_title：Archiv der Pharmazie

authors： Misiura K,Kardacka K,Kusnierczyk H

更新日期：2001-09-01 00:00:00

abstract：:A facile synthesis of a group of novel thiazole-pyrazolone hybrids and their investigation for angiotensin-converting enzyme (ACE) inhibition are reported in this study. These compounds were synthesized using a well-known approach, based on the condensation of ethyl acetoacetate with thiazolylhydrazines, and character...

journal_title：Archiv der Pharmazie

authors： You H,Su X,Su G

更新日期：2020-12-01 00:00:00

abstract：:Diverse biological activities have been found in compounds having a quinazolinone ring system. A large number of 4(3H)-quinazolinones, in particular those possessing 2-alkyl-3-aryl, 2,3-dialkyl, and 2-alkyl-3-amino substitution, have been evaluated for pharmacological activity. On the other hand, thiazolidone derivati...

journal_title：Archiv der Pharmazie

authors： el-Feky SA,Abd el-Samii ZK

更新日期：1991-06-01 00:00:00

abstract：:The synthesis and odour properties of the new santalol analogue, methyl-beta-santalol, are described. The additional methyl group adjacent to the hydroxyl function of the standard molecule, beta-santalol, deprives the new compound of the sandalwood note. The synthesis and the odour evaluation of this compound supports...

journal_title：Archiv der Pharmazie

authors： Buchbauer G,Zechmeister-Machhart F,Weiss-Greiler P,Wolschann P

更新日期：1997-04-01 00:00:00

abstract：:A 3D pharmacophore model predicting anticonvulsant activity was obtained for a series of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives recently disclosed as a new class of noncompetitive AMPA receptor antagonists. The training set included 17 compounds with varying potency against audiogenic seizures in DBA...

journal_title：Archiv der Pharmazie

authors： De Luca L,Gitto R,Barreca ML,Caruso R,Quartarone S,Citraro R,De Sarro G,Chimirri A

更新日期：2006-07-01 00:00:00

abstract：:This paper reports the synthesis of the new compound 1-[2-acetoxy-3-(4-phenyl-1-piperazinyl)propyl]pyrrolidin-2-one (Ac-MG-1). Preliminary pharmacological assessment revealed that Ac-MG-1 possesses anti-arrhythmic activity and a local anesthetic effect. The crystal structure of Ac-MG-1 was determined by X-ray diffract...

journal_title：Archiv der Pharmazie

authors： Malawska B,Filipek B,Stadnicka K,Ciechanowicz-Rutkowska M

更新日期：1995-06-01 00:00:00

abstract：:Antibiotic-resistant bacteria continue to play an important role in human health and disease. Inventive strategies are necessary to develop new therapeutic leads to challenge drug-resistance problems. From this perception, new quinoline hybrids bearing bioactive pharmacophores were synthesized. The newly synthesized c...

journal_title：Archiv der Pharmazie

authors： Rizk OH,Bekhit MG,Hazzaa AAB,El-Khawass EM,Abdelwahab IA

更新日期：2019-10-01 00:00:00

abstract：:Cathepsin B and plasmin are intra- or extracellular proteases that are overexpressed by several solid tumors. In order to exploit both proteases as molecular targets for tumor-specific cleavage of prodrugs, an albumin-binding formulation of methotrexate was developed that incorporated the peptide sequence D-Ala-Phe-Ly...

journal_title：Archiv der Pharmazie

authors： Warnecke A,Fichtner I,Sass G,Kratz F

更新日期：2007-08-01 00:00:00

abstract：:A new method for the synthesis of ODN-luciferase conjugate was investigated as a signal-amplifying sensor of the target nucleic acids. The conjugation of the luciferase was successfully achieved between the cysteine residue and the 2-amino-6-vinylpurine nucleoside of the ODN probe without significant inactivation of l...

journal_title：Archiv der Pharmazie

authors： Nagatsugi F,Nakahara R,Inoue K,Sasaki S

更新日期：2008-09-01 00:00:00

abstract：:Fourteen new 1-[(N, N-disubstituted thiocarbamoylthio)acetyl]-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives (7a-n) were synthesised by reacting 1-(chloroacetyl)-3-(2-thienyl)-5-aryl-2-pyrazolines (5a-g) and appropriate sodium salts of N, N-disubstituted dithiocarbamoic acids (6a, b). The structures of the synthesised ...

journal_title：Archiv der Pharmazie

authors： Turan-Zitouni G,Ozdemir A,Güven K

更新日期：2005-03-01 00:00:00

abstract：:The histone deacetylase (HDAC) enzyme plays an important role in gene transcription. Inhibitors of histone deacetylases induce cell differentiation and suppress cell proliferation in tumor cells. Hydroxamates with rigid linker have displayed better inhibition profiles than those with linear and flexible aliphatic link...

journal_title：Archiv der Pharmazie

authors： Chakrabarty S,Jasmine,Bhadaliya C,Sinha BN,Mahesh A,Bai H,Blond SY,Jayaprakash V

更新日期：2010-03-01 00:00:00

abstract：:The shock-induced serine protease HtrA1 is a potential regulator of human placenta development during pregnancy. The protein contains a functional PDZ domain that has been solved in complex with a phage display-derived heptapeptide: Asp-6 Ser-5 Arg-4 Ile-3 Trp-2 Trp-1 Val0 . In this study, a rationally designed haloge...

journal_title：Archiv der Pharmazie

authors： Dou SF,Liu H,Cao TM,Wen QL,Li J,Shao QC

更新日期：2016-04-01 00:00:00

abstract：:In an attempt to counteract bacterial pathogenicity, a set of novel imidazolidine-2,4-dione and 2-thioxoimidazolidin-4-one derivatives was synthesized and evaluated as inhibitors of bacterial virulence. The new compounds were characterized and screened for their effects on the expression of virulence factors of Pseudo...

journal_title：Archiv der Pharmazie

authors： Mohamed B,Abdel-Samii ZK,Abdel-Aal EH,Abbas HA,Shaldam MA,Ghanim AM

更新日期：2020-05-01 00:00:00

abstract：:Poly(vinyl alcohol) was crosslinked with ethylene glycol diglycidyl ether to obtain hydrogel-forming polymers. The polymers were also substituted with oleoyl chloride, providing hydrogels with weak solubility. These new polymeric materials were evaluated for the formulation of sustained drug delivery systems. Vancomyc...

journal_title：Archiv der Pharmazie

authors： Orienti I,Treré R,Luppi B,Bigucci F,Cerchiara T,Zuccari G,Zecchi V

更新日期：2002-03-01 00:00:00

abstract：:MXT-M-3,2 breast cancer implanted into female B6D2F1 mice accelerates the growth of an identical second tumor. This process is accompanied by a significant increase of the granulocyte and monocyte numbers in the blood and of the granulocyte and macrophage numbers in the spleen. A significant positive correlation of st...

journal_title：Archiv der Pharmazie

authors： Schlemmer R,Spruss T,Bernhardt G,Schönenberger H

更新日期：2000-12-01 00:00:00

abstract：:A series of homochiral 7-substituted 1-aminoindans was prepared by means of asymmetric reductive amination from racemic 7-substituted 1-indanones via E-imines and E-imine/enamine mixtures, respectively, and subjected to 5-hydroxytryptamine (5-HT) receptor subtype binding studies. The ee's of the title compounds were d...

journal_title：Archiv der Pharmazie

authors： Landsiedel-Maier D,Frahm AW

更新日期：1998-02-01 00:00:00

abstract：:The aim of this study was to develop a novel nanosize drug candidate for cancer therapy. For this purpose, (S)-methyl 2-[(7-hydroxy-2-oxo-4-phenyl-2H-chromen-8-yl)methyleneamino]-3-(1H-indol-3-yl)propanoate (ND3) was synthesized by the condensation reaction of 8-formyl-7-hydroxy-4-phenylcoumarin with l-tryptophan meth...

journal_title：Archiv der Pharmazie

authors： Budama-Kilinc Y,Kecel-Gunduz S,Ozdemir B,Bicak B,Akman G,Arvas B,Aydogan F,Yolacan C

更新日期：2020-11-01 00:00:00

abstract：:Cancer can invade or spread to almost all parts of the body. The increasing morbidity and high mortality of cancer create a great demand for the development of novel anticancer drugs. Coumarin derivatives are ubiquitous in nature and can readily interact with diverse enzymes and receptors in cancer cells via weak bond...

journal_title：Archiv der Pharmazie

authors： Song XF,Fan J,Liu L,Liu XF,Gao F

更新日期：2020-08-01 00:00:00

abstract：:A novel dimer of 2-(4-pyridylmethyl)-1-indanone (2) was obtained while carrying out aldol condensation of 1-indanone with pyridine-4-carboxaldehyde in potassium hydroxide. The structure of dimer 3 has been established using various spectral techniques and was screened for its ability to inhibit the cytochrome P(450) e...

journal_title：Archiv der Pharmazie

authors： Gupta R,Jindal DP,Jit B,Narang G,Palusczak A,Hartmann RW

更新日期：2004-07-01 00:00:00

abstract：:A short series of arylhydrazones of 4-[(2-methylimidazo[1,2-a]pyridine-3-yl)azo]benzoic acid hydrazide was synthesized and tested for antimicrobial activity. All of the compounds show antimicrobial activity against Escherichia coli. A few members were also active against Klebsiella pneumoniae, Staphylococcus aureus an...

journal_title：Archiv der Pharmazie

authors： Cesur Z,Büyüktimkin S,Büyüktimkin N,Derbentli S

更新日期：1990-03-01 00:00:00

abstract：:Synthesis of some new derivatives of 2-aryl-4-oxo-1-(4-quinazolyl)quinazolines is described. Methyl N-(4-quinazolyl)anthranilate was allowed to react with phenyl iso(thio)cyanate to give 3-phenyl-1-(4-quinazolyl)-1, 2, 3, 4-tetrahydro-2, 4-dioxo- and 4-oxo-2-thioxoquinazolines (3a and 3b respectively) Alternatively, a...

journal_title：Archiv der Pharmazie

authors： Gineinah MM,El-Sherbeny MA,Nasr MN,Maarouf AR

更新日期：2002-01-01 00:00:00

abstract：:New, non-imidazole histamine H3 receptor antagonists were prepared and in vitro tested as H3 receptor antagonists measured as the electrically evoked contraction of the guinea-pig jejunum. The 2-(1-piperidinyl)- and 2-(1-pyrrolidinyl)benzothiazoles show no or very poor activity; 2-[1-(4-amino)piperidinyl]- and 2-(1,2-...

journal_title：Archiv der Pharmazie

authors： Walczyński K,Guryn R,Zuiderveld OP,Timmerman H

更新日期：1999-11-01 00:00:00

abstract：:A range of novel pyridine-2,4,6-tricarbohydrazide thiourea compounds (4a-i) were synthesized in good to excellent yields (63-92%). The enzyme inhibitory potentials of these compounds were investigated against α- and β-glucosidases because these enzymes play a crucial role in treating type-2 diabetes mellitus (T2DM). A...

journal_title：Archiv der Pharmazie

authors： Rehman TU,Riaz S,Khan IU,Ashraf M,Bajda M,Gawalska A,Yar M

更新日期：2018-01-01 00:00:00

abstract：:The syntheses, conformational studies, and investigations on the estrogen receptor binding of [R/S-1-(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]platinum(II) complexes (1-PtL2, 2L = leaving groups) are described. A Strecker synthesis using the 2,6-dichloro-4-methoxybenzaldehyde, NaCN, and NH4Cl afforded the cyanoami...

journal_title：Archiv der Pharmazie

authors： Gust R,Lubczyk V,Schmidt K,Shihada U

更新日期：2001-03-01 00:00:00

abstract：:In this study, we have explored the prevention of gastric side effects such as gastric lesions and bleeding while maintaining the high analgesic and anti-inflammatory activities by the derivatization of the carboxylate moiety into amides in [5-chloro-6-(2-chloro/fluorobenzoyl)-2-benzoxazolinone-3-yl]acetic acids. We h...

journal_title：Archiv der Pharmazie

authors： Banoglu E,Okçelik B,Kupeli E,Unlü S,Yeşilada E,Amat M,Caturla JF,Sahin MF

更新日期：2003-07-01 00:00:00

abstract：:A series of 5-amino-3-methylisoxazole-4-carboxylic acid amides has been prepared by condensation of 5-amino-3-methylisoxazole-4-carboxylic acid with ethyl chloroformate. The resulting mixed anhydride undergoes condensation with appropriate phenylamides to form the corresponding amides 6-16. The compounds obtained were...

journal_title：Archiv der Pharmazie

authors： Ryng S,Zimecki M,Sonnenberg Z,Mokrosz MJ

更新日期：1999-05-01 00:00:00

abstract：:Starting from L-aspartic acid the preparation of 8-aminopyrido[1,2-a]indole derivatives as benzo-fused analogs of the dopamine autoreceptor agonist 1 is reported. The key step of the synthesis is the Tf2O induced cyclization of the 1,2-amino alcohol 6. Receptor binding studies indicated selective affinity for the D-2 ...

journal_title：Archiv der Pharmazie

authors： Gmeiner P,Kärtner A,Mierau J

更新日期：1995-07-01 00:00:00

abstract：:Structural feature analysis of chlorogenic acid derivatives made up of varying lengths of alkyl groups as α-glucosidases inhibitors were performed by QSAR techniques. The statistically significant models derived from the study were validated by leave one out, Y-randomization and test set methods. The predictive capaci...

journal_title：Archiv der Pharmazie

authors： Narayana Moorthy NS,Ramos MJ,Fernandes PA

更新日期：2012-04-01 00:00:00

abstract：:3-Amino-1,4-benzodiazepines as well as chemically related diverse amines were prepared from oxazepam and subsequently screened on the cholecystokinin receptor in a radiolabel binding assay. Oxazepam 2 was activated via its 3-chloro-1,4-benzodiazepine intermediate 3 and was reacted with a large series of aliphatic and ...

journal_title：Archiv der Pharmazie

authors： Offel M,Lattmann P,Singh H,Billington DC,Bunprakob Y,Sattayasai J,Lattmann E

更新日期：2006-04-01 00:00:00

abstract：:Polyketide-derived macrolactones like zearalenone (1), zearalane (2) or curvularin (3) display a wide range of interesting pharmacological activities. Here, we present a short and efficient approach towards this class of natural products by a combination of the Sonogashira and Mitsunobu reactions. The resulting lacton...

journal_title：Archiv der Pharmazie

authors： Krauss J,Unterreitmeier D,Neudert C,Bracher F

更新日期：2005-12-01 00:00:00