Design, synthesis, and molecular docking of novel indole scaffold-based VEGFR-2 inhibitors as targeted anticancer agents.

abstract：:Marine organisms play an important role in natural product-based drug research due to accumulation of structurally unique and bioactive metabolites. The exploration of marine-derived compounds may significantly extend the scientific knowledge of potential scaffolds for antibiotic drug discovery. Development of novel a...

journal_title：Archiv der Pharmazie

authors： Daletos G,Ancheeva E,Chaidir C,Kalscheuer R,Proksch P

更新日期：2016-10-01 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：:A series of novel 2,4-disubstituted 7-methyl-1,1,3-trioxo-2,4-dihydro-pyrazolo[4,5-e] [1,2,4]thiadiazines (PTDs) was synthesized, structurally confirmed by spectral analysis, and evaluated for their anti-HIV activities by inhibition of HIV-induced cytopathogenicity in MT-4 cell culture. The results showed that some co...

journal_title：Archiv der Pharmazie

authors： Liu XY,Yan RZ,Wang Y,Zhan P,De Clercq E,Pannecouque C,Witvrouw M,Molina MT,Vega S

更新日期：2008-04-01 00:00:00

abstract：:A novel series of hybrid molecules 4a-i and 5a-i were prepared by condensation of 4-(trimethylsilylethynyl)benzaldehyde 1 with substituted o-phenylenediamines. These in turn were reacted with 2-(azidomethoxy)ethyl acetate in a Cu alkyne-azide cycloaddition (CuAAC) to generate the 1,2,3-triazole pharmacophore under mic...

journal_title：Archiv der Pharmazie

authors： Ouahrouch A,Ighachane H,Taourirte M,Engels JW,Sedra MH,Lazrek HB

更新日期：2014-10-01 00:00:00

abstract：:New analogues of nifedipine, in which the 2-nitrophenyl group at position 4 is replaced by a 1-methyl-5-nitro-2-imidazolyl substituent, were synthesized. The symmetrical dialkyl 1, 4-dihydro-2, 6-dimethyl-4-(1-methyl-5-nitro-2-imidazolyl)-3, 5-pyridinedicarboxylates were prepared by a classical Hantzsch condensation. ...

journal_title：Archiv der Pharmazie

authors： Miri R,Javidnia K,Kebriaie-Zadeh A,Niknahad H,Shaygani N,Semnanian S,Shafiee A

更新日期：2003-09-01 00:00:00

abstract：:1-deoxy-D-xylulose-5-phosphate reductoisomerase (Dxr) represents an essential enzyme of the mevalonate-independent pathway of the isoprenoid biosynthesis. Using fosmidomycin as a specific inhibitor of Dxr, this enzyme was previously validated as target for the treatment of malaria and bacterial infections. The replace...

journal_title：Archiv der Pharmazie

authors： Ortmann R,Wiesner J,Silber K,Klebe G,Jomaa H,Schlitzer M

更新日期：2007-09-01 00:00:00

abstract：:Stress is implicated in the pathogenesis of numerous disorders such as cardiovascular diseases or neurodegeneration. The extensive overlap between diseases attributed to stress and oxidative damage is indicative of their potential relationship. We hereby study the influence of alpha-tocopherol (alpha-toc) on the devel...

journal_title：Archiv der Pharmazie

authors： Tsiakitzis K,Kourounakis AP,Tani E,Rekka EA,Kourounakis PN

更新日期：2005-07-01 00:00:00

abstract：:Numerous novel N,N-disubstituted 5-alkyliden- or 5-aralkyliden-3-aminorhodanines 2 have been prepared by condensation of carbonyl compounds with 1. The effectiveness of some derivatives in an "akanthose test" with hairless mice was shown. ...

journal_title：Archiv der Pharmazie

authors： Hanefeld W,Helfrich V,Jalili MA,Schlitzer M

更新日期：1993-06-01 00:00:00

abstract：:A series of 3,4-bis-chalcone-N-arylpyrazoles 3a-k was prepared from diacetyl pyrazoles 2a-e. The reaction of 2d and 2e with hydrazine hydrate gave pyrazolo[3,4-d]pyridazine derivatives 4a-b. Furthermore, the reaction of 2a-e with thiosemicarbazide afforded pyrazolo[3,4-d]pyridazine thiocyanate salts 5a-e. The synthesi...

journal_title：Archiv der Pharmazie

authors： El-Sabbagh OI,Mostafa S,Abdel-Aziz HA,Ibrahim HS,Elaasser MM

更新日期：2013-09-01 00:00:00

abstract：:3-Ethyl 5-methyl 1,4-dihydro-2-[(2-hydroxyethoxy) methyl]-6-methyl-4-(2,3-dichlorophenyl)-3,5-pyridinedicarboxylate (13), a bioisostere of amlodipine, was prepared by the reaction of ethyl 4-(2-hydroxyethoxy)acetoacetate (11) with methyl 2-(2,3-dichlorobenzylidene)acetoacetate (12) and NH4OAc. Compound 13 was elaborat...

journal_title：Archiv der Pharmazie

authors： Yiu SH,Knaus EE

更新日期：1999-10-01 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：: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：:A series of 4-amino-7,8-dimethoxy-5H-pyrimido[5,4-b]indole derivatives has been synthesized. These compounds resemble carbazeram and other pyridazino compounds with activity in the cardiovascular system. Some of these new compounds possess inotropic activity (Table 2), with a complementary effect on the inhibition of ...

journal_title：Archiv der Pharmazie

authors： Monge A,Martínez-Crespo FJ,Villanueva MA,Font M,Santiago E,Martínez de Irujo JJ,Alberdi E,López-Unzu MJ,Cenarruzabeitia E,Castiella E

更新日期：1993-11-01 00:00:00

abstract：:Prevention of the formation of advanced glycation end-products (AGEs) is a reliable approach to achieve control over hyperglycemia and the associated pathogenesis of diabetic vascular complications. In these terms, new synthetic approaches to 6-nitroazolo[1,5-a]pyrimidines have been developed on the basis of the promi...

journal_title：Archiv der Pharmazie

authors： Spasov AA,Babkov DA,Sysoeva VA,Litvinov RA,Shamshina DD,Ulomsky EN,Savateev KV,Fedotov VV,Slepukhin PA,Chupakhin ON,Charushin VN,Rusinov VL

更新日期：2017-12-01 00:00:00

abstract：:A series of eperezolid analogs with glycinyl substitutions were prepared and their antibacterial activities were studied against a panel of susceptible and resistant Gram-positive bacteria. The compounds with N-arylacyl or N-heteroarylacyl glycinyl structural units showed good antibacterial activities. The compounds 1...

journal_title：Archiv der Pharmazie

authors： Wang XJ,Wu N,Du GJ,Zhao SQ,Yan M,Gu LQ

更新日期：2009-07-01 00:00:00

abstract：:Increases in the intracellular levels of glutathione (GSH) in cancer cells have been implicated in the development of acquired resistance to platinum antitumor agents. On the other hand, little information is available on the relationships between intracellular GSH levels in non-treated cancer cells and their response...

journal_title：Archiv der Pharmazie

authors： Boubakari,Bracht K,Neumann C,Grünert R,Bednarski PJ

更新日期：2004-12-01 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 precise definition of the structural requirements for effective topoisomerase II poisoning by drug molecules is still an elusive issue. In the attempt to better define a pharmacophoric pattern, we prepared several conjugates combining the chemical features of two well-known topoisomerase II poisons, amsacrine and ...

journal_title：Archiv der Pharmazie

authors： Zagotto G,Gianoncelli A,Sissi C,Marzano C,Gandin V,Pasquale R,Capranico G,Ribaudo G,Palumbo M

更新日期：2014-10-01 00:00:00

abstract：:The preparation and detailed composition of an oil newly extracted from pure soy germ (not less than 96 % hypocotyle) are presented. Experiments in vivo showed that soybean-germ oil (SGO) possesses a remarkable protective activity against UVB-induced skin inflammation, exceeding that of tocopherol acetate by a factor ...

journal_title：Archiv der Pharmazie

authors： Bonina F,Puglia C,Avogadro M,Baranelli E,Cravotto G

更新日期：2005-12-01 00:00:00

abstract：:To identify new agents for the treatment of American cutaneous leishmaniasis, a series of eight 1,4-bis(substituted benzalhydrazino)phthalazines was evaluated against Leishmania braziliensis and Leishmania mexicana parasites. These compounds represent a disubstituted version of the 1-chloro-4-(monoaryl/heteroarylhydra...

journal_title：Archiv der Pharmazie

authors： Romero AH,Rodríguez N,Oviedo H,Lopez SE

更新日期：2019-06-01 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：:The present work describes the synthesis and antifungal evaluation of new 5-arylidene-(Z)-2-dimethylamino-1,3-thiazol-4-ones 4a-f, obtained by the reaction of aromatic aldehydes 1 and rhodanine 2 followed by treatment with DMF. All compounds were tested against a panel of yeasts, hialohyphomycetes, and dermatophytes u...

journal_title：Archiv der Pharmazie

authors： Insuasty B,Gutiérrez A,Quiroga J,Abonia R,Nogueras M,Cobo J,Svetaz L,Raimondi M,Zacchino S

更新日期：2010-01-01 00:00:00

abstract：:The diffusion of a series of non steroidal antiinflammatory drugs through a silicone rubber membrane has been studied from suspensions both of the free and beta-cyclodextrin complexes forms at different pH values of the medium. Higher diffusion rates of the complexed forms as compared with the free ones and a rate-lim...

journal_title：Archiv der Pharmazie

authors： Orienti I,Cavallari C,Zecchi V,Fini A

更新日期：1989-04-01 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 objective of this work was to develop a liver-specific antihepato carcinoma agent. A series of 5-fluorouracil / cholic acid conjugates (5-FU-cholic acid conjugates) were prepared and tested for their chemical characteristics and bio-distribution properties. The in-vitro stability trial showed 5-FU-cholic acid conj...

journal_title：Archiv der Pharmazie

authors： Qian S,Wu JB,Wu XC,Li J,Wu Y

更新日期：2009-09-01 00:00:00

abstract：:A series of 1-¿omega-(4-aryl-1-piperazinyl)alkyl]indolin-2(1H)-one derivatives 2-14 was synthesized in order to obtain ligands with a dual 5-HT1A/5-HT2A activity. The majority of those compounds (2-5, 7, 10-13) exhibited a high 5-HT1A (Ki = 2-44 nM) and/or 5-HT2A affinity (Ki = 51 and 39 for 5 and 7, respectively). In...

journal_title：Archiv der Pharmazie

authors： Mokrosz MJ,Duszyńska B,Misztal S,Kłodzińska A,Tatarczyńska E,Chojnacka-Wójcik E,Dziedzicka-Wasylewska M

更新日期：1998-10-01 00:00:00

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：: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 synthesis of 4-Methoxyphenyl-[5-methyl-6-(2-(4-morpholinyl)-ethyl)-6H-thieno[2,3- b]pyrrol-4-yl)phenylmethanone (1), a thiophene analogue of the analgesic Pravadoline B, is described. Starting with the acetylprotected thienylhydrazine 2b compound 7 was obtained in a Fischer-analogue cyclication in two steps. Use o...

journal_title：Archiv der Pharmazie

authors： Binder D,Schnait H,Rovenszky F,Enzenhofer R,Stroissnig H

更新日期：1991-04-01 00:00:00

abstract：:Two new arylnaphthalide lignans, procumphthalide A (1) and 4-O-beta-D-glucopyranosyl-(1"'-->2")-beta-D-apiofuranosyldiphyllin, named procumbenoside B (2), along with cilinaphthalide B (3) and several other known compounds were isolated from the methanolic extracts of Justicia procumbens. By using NMR and other spectra...

journal_title：Archiv der Pharmazie

authors： Weng JR,Ko HH,Yeh TL,Lin HC,Lin CN

更新日期：2004-04-01 00:00:00