Synthesis and evaluation of the luciferase-oligodeoxynucleotide for the sequence-selective detection of nucleic acids.

abstract：:Several chloro- and iodo-lignanolides have been obtained by direct halogenation of aromatic rings from yatein and 4'-O-demethylyatein. They were assayed as antineoplastics, in order to check the influence in the activity of substitution in both aromatic rings. Although these compounds show a modest antineoplastic acti...

journal_title：Archiv der Pharmazie

authors： Medarde M,Peláez-Lamamié de Clairac R,López JL,Grávalos DG,San Feliciano S

更新日期：1995-09-01 00:00:00

abstract：:JL 13 (5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b]- [1,5]benzoxazepine fumarate) and JL 3 (10-(4-methylpiperazin-1- yl)pyrido[4,3-b][1,4]benzothiazepine), two pyridobenzazepine derivatives structurally related to clozapine, were selected for further development. Due to their structural similarity to clozapine, t...

journal_title：Archiv der Pharmazie

authors： Liégeois JF,Zahid N,Bruhwyler J,Uetrecht J

更新日期：2000-03-01 00:00:00

abstract：:A series of new positive inotropic agents was synthesized with the aim of combining the pharmacophores of the imidazolone-type phosphodiesterase (PDE) inhibitor enoximone and guanidine-type histamine H2 receptor agonists such as arpromidine. All compounds are para-substituted 4-benzoyl-5-alkyl-2-imidazolones. H2 agoni...

journal_title：Archiv der Pharmazie

authors： Glass D,Buschauer A,Tenor H,Bartel S,Will-Shahab L,Krause EG

更新日期：1995-10-01 00:00:00

abstract：:In accordance with the significant impetus of the discovery of potent vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitors, herein, we report the design, synthesis, and anticancer evaluation of 12 new N-substituted-4-phenylphthalazin-1-amine derivatives against HepG2, HCT-116, and MCF-7 cells as VEGFR-2 ...

journal_title：Archiv der Pharmazie

authors： El-Adl K,Ibrahim MK,Khedr F,Abulkhair HS,Eissa IH

更新日期：2020-11-16 00:00:00

abstract：:The oncoprotein cytotoxic associated gene A (CagA) of Helicobacter pylori plays a pivotal role in the development of gastric cancer, so it has been an important target for anti-H. pylori drugs. Conventional drugs are currently being implemented against H. pylori. The inhibitory role of plant metabolites like curcumin ...

journal_title：Archiv der Pharmazie

authors： Srivastava AK,Tewari M,Shukla HS,Roy BK

更新日期：2015-08-01 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：:The synthesis and the pharmacological activity of a series of 1-aroyl derivatives of kynurenic acid methyl ester (4-oxo-quinolin-2-carboxy methyl (KYNA) esters), structurally related to NSAID indomethacin are described. The derivatives were screened in vivo for anti-inflammatory and analgesic activities. Most of the c...

journal_title：Archiv der Pharmazie

authors： Mazzoni O,Esposito G,Diurno MV,Brancaccio D,Carotenuto A,Grieco P,Novellino E,Filippelli W

更新日期：2010-10-01 00:00:00

abstract：:A novel series of N-(2-(piperazin-1-yl)phenyl)aryl carboxamide derivatives were simply synthesized by Ugi-multicomponent reaction as β-secretase (BACE1) inhibitors. The BACE1 inhibitory activity of the synthesized compounds was examined using a Forester resonance energy transfer (FRET)-based assay. Among the tested co...

journal_title：Archiv der Pharmazie

authors： Edraki N,Firuzi O,Fatahi Y,Mahdavi M,Asadi M,Emami S,Divsalar K,Miri R,Iraji A,Khoshneviszadeh M,Firoozpour L,Shafiee A,Foroumadi A

更新日期：2015-05-01 00:00:00

abstract：:Synthesis of a new series of 1beta-methylcarbapenems with a substituted oxadiazolopyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of the substituent on the oxadiazole ring investigated. In particular, compounds 13...

journal_title：Archiv der Pharmazie

authors： Oh CH,Dong HG,Lee JS,Lee SC,Hong JH,Cho JH

更新日期：2003-12-01 00:00:00

abstract：:Three novel series of quinoline derivatives have been prepared by cyclization of the intermediate 3-(1,3-dioxolan-2-yl)-2-substituted thiocarbamoyl-hydrazinoquinolines with different alpha-halocarbonyl compounds. These series are: 3-(1,3-dioxolan-2-yl)-2-(3-substituted-4-phenylthiazolin-2-y lidene) hydrazinoquinolines...

journal_title：Archiv der Pharmazie

authors： Farghaly AM,Habib NS,Khalil MA,el-Sayed OA,Bistawroos AE

更新日期：1990-04-01 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：:Phosphono-analogues of glutathione containing the O = P(OR)2 moiety in place of the cysteinyl residue CH2SH 1a-1d were prepared by solution phase peptide synthesis. Benzyl, benzyloxy-carbonyl, and tert-butyl protecting groups were used to mask the individual amino acid functional groups. The formation of peptide bonds...

journal_title：Archiv der Pharmazie

authors： Kunze T

更新日期：1996-11-01 00:00:00

abstract：:Schistosoma mansoni histone deacetylase 8 (SmHDAC8) has been recently identified as a new potential target for the treatment of schistosomiasis. A series of newly designed and synthesized alkoxyamide-based and hydrazide-based HDAC inhibitors were tested for inhibitory activity against SmHDAC8 and human HDACs 1, 6, and...

journal_title：Archiv der Pharmazie

authors： Stenzel K,Chakrabarti A,Melesina J,Hansen FK,Lancelot J,Herkenhöhner S,Lungerich B,Marek M,Romier C,Pierce RJ,Sippl W,Jung M,Kurz T

更新日期：2017-08-01 00:00:00

abstract：:A rapid and efficient one-pot condensation reaction of long-chain alkyl and alkenyl acid hydrazides and nitriles was carried out to afford 3,5-disubstituted-1H-1,2,4-triazoles. The compounds 5a-o were screened for in-vitro antibacterial activity against the representative panel of two Gram-positive and two Gram-negati...

journal_title：Archiv der Pharmazie

authors： Sharma S,Gangal S,Rauf A,Zahin M

更新日期：2008-11-01 00:00:00

abstract：:A series of dialkyl, dicycloalkyl, and diaryl ester analogues of nifedipine, in which the ortho-nitro phenyl group at position 4 is replaced by the 4-(5)-chloro-2-ethyl-5-(4)-imidazolyl substituent, were synthesized and evaluated as calcium channel antagonists using the high K+ contraction of guinea pig ileal longitud...

journal_title：Archiv der Pharmazie

authors： Davood A,Mansouri N,Rerza Dehpour A,Shafaroudi H,Alipour E,Shafiee A

更新日期：2006-06-01 00:00:00

abstract：:The aim of our study was to investigate structure activity relationship following the replacement of the 6-phenyl substituent at the 6,7-diaryl-2,3-dihydropyrrolizine template by various heteroaromatic residues. In this context we developed a new, efficient, and highly sensitive test method for the screening of dual c...

journal_title：Archiv der Pharmazie

authors： Laufer S,Striegel HG,Neher K,Zechmeister P,Donat C,Stolingwa K,Baur S,Tries S,Kammermeier T,Dannhardt G,Kiefer W

更新日期：1997-10-01 00:00:00

abstract：:The pyrrolidino enaminones, with the carboxylic acid chain fixed at the nitrogen, inhibit cyclooxygenase more potently or selectively than 5-lipoxygenase. According to the structure-activity relationships discussed the potency depends significantly on the chain length of the carboxylic acid, the substitution pattern o...

journal_title：Archiv der Pharmazie

authors： Dannhardt G,Bauer A,Nowe U

更新日期：1997-03-01 00:00:00

abstract：:A new series of 1,2,4-triazolo[4,3-c]quinazoline derivatives was designed and synthesized as Topo II inhibitors and DNA intercalators. The cytotoxic effect of the new members was evaluated in vitro against a group of cancer cell lines including HCT-116, HepG-2, and MCF-7. Compounds 14c , 14d , 14e , 14e , 15b , 18b , ...

journal_title：Archiv der Pharmazie

authors： Alesawy MS,Al-Karmalawy AA,Elkaeed EB,Alswah M,Belal A,Taghour MS,Eissa IH

更新日期：2020-11-23 00:00:00

abstract：:This review emphasizes the relationship of breast cancer, estrogen receptor and ligands, especially the centrality of the estrogen receptor, which mediates on one hand the hormone-induced gene transcription and on the other hand the anti-estrogen action against breast cancer. The characterization of the estrogen recep...

journal_title：Archiv der Pharmazie

authors： Bai Z,Gust R

更新日期：2009-03-01 00:00:00

abstract：:Chemical modification of cinnoxacin was studied with the aim of improving its antibacterial activity and spectrum. A series of 4-imino-1, 4-dihydrocinnoline-3-carboxylic acid derivatives was synthesized and their in vitro antibacterial activity was evaluated. These derivatives were designed as isosteric analogues of f...

journal_title：Archiv der Pharmazie

authors： Stańczak A,Ochocki Z,Martynowski D,Główka M,Nawrot E

更新日期：2003-03-01 00:00:00

abstract：:The ongoing interest in very efficient systems for the imitation of cytochrome P-450-dependent monooxygenase reactions, consisting of metalloporphyrin and oxygen donor, prompted us to develop a method to compare the catalytic activity of soluble metalloporphyrins with those which have been immobilised on different sil...

journal_title：Archiv der Pharmazie

authors： Lübbe AN,Rickerts B,Duchstein HJ

更新日期：2006-12-01 00:00:00

abstract：:New 5-(2-arylethenyl)-1, 2, 4-triazine N-oxide and N, N'-dioxide derivatives were synthesized in order to obtain compounds as selective hypoxic cell cytotoxins. The desired products were obtained when the 5-methyl heterocycle reacted with the corresponding iminium electrophiles. The new compounds were tested for their...

journal_title：Archiv der Pharmazie

authors： Cerecetto H,González M,Risso M,Saenz P,Olea-Azar C,Bruno AM,Azqueta A,De Ceráin AL,Monge A

更新日期：2004-05-01 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：:1-Substiuted 6-(3-cyanobenzoyl) and [(3-cyanophenyl)fluoromethyl]-5-ethyl-uracils were synthesized and evaluated in cell-based assays against HIV-1 wild-type and its clinically relevant non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant mutants. Some of the synthesized compounds showed activity against H...

journal_title：Archiv der Pharmazie

authors： Loksha YM,Pedersen EB,Loddo R,La Colla P

更新日期：2009-09-01 00:00:00

abstract：:Paullones 3 and 4 with aminoalkyl side chains in 2- or 3-position were synthesized as derivatives of kenpaullone 1. Both 3 and 4 showed the characteristic CDK1-inhibitory activity of the paullones and a modest antiproliferative activity on cultured human tumor cell lines. Hence, 3 and 4 appear to be suitable tools for...

journal_title：Archiv der Pharmazie

authors： Wieking K,Knockaert M,Leost M,Zaharevitz DW,Meijer L,Kunick C

更新日期：2002-07-01 00:00:00

abstract：:Nine novel acyl thioureas were synthesized. Their identities and purities were confirmed by LC-MS spectra; each structure was elucidated by elemental analysis, IR, 1 Н and 13 C NMR spectra. Applying an in vitro screening of their antifungal potential, three substances (3, 5, and 6) could be selected as showing high ac...

journal_title：Archiv der Pharmazie

authors： Antypenko L,Meyer F,Kholodniak O,Sadykova Z,Jirásková T,Troianova A,Buhaiova V,Cao S,Kovalenko S,Garbe LA,Steffens KG

更新日期：2019-02-01 00:00:00

abstract：:The newly synthesized analogs of NAN-190 containing m-Cl and m-CF(3) substituents in the arylpiperazine moiety and their conformationally restricted counterparts showed a very high 5-HT(1A )receptor affinity. In the LLR test, the flexible compounds 4a and 5a displayed features of a partial agonist and agonist, respect...

journal_title：Archiv der Pharmazie

authors： Paluchowska MH,Bugno R,Charakchieva-Minol S,Bojarski AJ,Tatarczyńska E,Chojnacka-Wójcik E

更新日期：2006-09-01 00:00:00

abstract：:Despite cellular complexity, a limited number of small molecules act as intracellular second messengers. Protein kinase A (PKA) is the main transducer of the information carried by cyclic adenosine monophosphate (cAMP). Recently, cellular imaging has achieved major technical advancements, although the search for more ...

journal_title：Archiv der Pharmazie

authors： Ribaudo G,Zagotto G,Ongaro A,Ricci A,Caretta A,Mucignat-Caretta C

更新日期：2020-04-01 00:00:00

abstract：:6-(1-Acyloxyalkyl)-5,8-dimethoxy-1,4-naphthoquinone (DMNQ; 5,8-dimethoxy-1,4-naphthoquinone) derivatives were synthesized and examined for their inhibitory effect on DNA topoisomerase-I (Topo I) and their antiproliferative activity against L1210 cells. The Topo-I inhibitory effect of 6-(1-hydroxyalkyl)-DMNQ derivative...

journal_title：Archiv der Pharmazie

authors： Kim Y,You YJ,Ahn BZ

更新日期：2001-10-01 00:00:00

abstract：:The key step in the synthesis of the pharmacologically interesting 1-phenyltetrahydro-3-benzazepine skeleton is the Michael addition of (2-lithiophenyl)acetaldehyde acetals, which are generated in situ upon treatment of the bromo acetals 5a,b with n-butyllithium, to beta-nitrostyrene (6). The reductive ring closure of...

journal_title：Archiv der Pharmazie

authors： Wünsch B,Nerdinger S,Bauschke G,Höfner G

更新日期：1997-07-01 00:00:00