Synthesis and biological evaluation of 5-arylfuro[2,3-d]pyrimidines as novel dihydrofolate reductase inhibitors.

abstract：:(+)-6-(2-Chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4, 5-tetrahydro-8H-pyrido[4',3':4,5]thieno[3,2-f]triazolo[4,3-a] [1,4]diazepine (E6123) is a very potent platelet-activating factor (PAF) receptor antagonist and shows potent anti-PAF activities at the microgram level in a variety of animal models. In ord...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazawa S,Okano K,Kawahara T,Machida Y,Yamatsu I

更新日期：1992-03-01 00:00:00

abstract：:A new spiroketallactone, epi-danshenspiroketallactone A (1) and a new C18-norditerpenoid, normiltioane (2) along with 21 known compounds, were isolated from cell cultures of Salvia miltiorrhiza. Their structures were elucidated on the basis of extensive spectroscopic analyses. In the in vitro assays, the compounds 9-1...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang DW,Liu X,Xie D,Chen R,Tao XY,Zou JH,Dai J

更新日期：2013-01-01 00:00:00

abstract：:The aim of this study was to evaluate the effects of Magnolin (MGL) on inhibition of human breast cancer cells, and explore the underlying molecular mechanisms. The viability of the treated cells was assessed with the Cell Counting Kit-8 (CCK-8) assay, and the proliferation was analyzed in terms of EdU uptake, colony ...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang J,Zhang S,Huang K,Shi L,Zhang Q

更新日期：2020-01-01 00:00:00

abstract：:We synthesized the racemates of the five presumed metabolites (1b-f) of (S)-(--)-N-tert-butyl-4,4-diphenyl-2-cyclopentenylamine hydrochloride (FK584, S(--)-1a), a novel agent for the treatment of overactive detrusor syndrome, in order to confirm the structures of the metabolites and also to evaluate their inhibitory a...

journal_title：Chemical & pharmaceutical bulletin

authors： Taniguchi K,Miyao Y,Yamano K,Yamamoto T,Terai T,Kusunoki T,Tsubaki K,Shiokawa Y

更新日期：1996-06-01 00:00:00

abstract：:A series of novel benzo[4,5]canthin-6-ones, bearing the N'-(substituted benzylidene)-carbohydrazide (11a-e) and N-alkylcarboxamide (13a-g) moieties at position-2, were synthesized and screened for their in vitro antitumor activity, against seven human cancer cell lines, and for antitrypanosomal and antileishmanial act...

journal_title：Chemical & pharmaceutical bulletin

authors： Leite Silva CM,Garcia FP,Rodrigues JH,Nakamura CV,Ueda-Nakamura T,Meyer E,Ruiz AL,Foglio MA,de Carvalho JE,da Costa WF,Sarragiotto MH

更新日期：2012-01-01 00:00:00

abstract：:Novel nucleoside analogues of structure 3-5 were synthesized starting from (+/-)-cis-2-amino-3-cyclopentenylmethanol (1). The chlorine derivative 3 inhibited both HIV-1 and HIV-2 replication in MT-4 cells with IC(50) values of 10.67 microM and of 13.79 microM, respectively. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Canoa P,González-Moa MJ,Teijeira M,Terán C,Uriarte E,Pannecouque C,De Clercq E

更新日期：2006-10-01 00:00:00

abstract：:We studied a method of estimating the number of contacts in a solid dosage form using thermal analysis. Ibuprofen (IB) and Ethenzamide (ET) were used as model actives. IB and ET were granulated and sieved with each other. We prepared mixtures of IB and ET using different diameter granules. The number of contacts betwe...

journal_title：Chemical & pharmaceutical bulletin

authors： Aoki S,Mizutani T,Danjo K

更新日期：2000-01-01 00:00:00

abstract：:In this study, we describe a highly selective etherification procedure of unprotected morroniside catalyzed by molecular iodine in acetone. The etherification reaction furnished 7-O-alkyl ether derivatives in reasonable yields within few hours under neutral conditions. Studies of the obtained products on cytotoxicity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Sunghwa F,Sakurai H,Saiki I,Koketsu M

更新日期：2009-01-01 00:00:00

abstract：:Rapid and precise compositional analysis of copoly (DL-lactic/glycolic acid) (PLGA) was performed by pyrolysis-gas chromatography/mass spectrometry (Py-GC/MS) combined with one-step hydrolysis and methylation in the presence of tetramethylammonium hydroxide (TMAH). Pyrolysis of PLGA with TMAH gave two characteristic p...

journal_title：Chemical & pharmaceutical bulletin

authors： Urakami K,Higashi A,Umemoto K,Godo M,Watanabe C,Hashimoto K

更新日期：2001-02-01 00:00:00

abstract：:To investigate the effect of the hot water extract from Artemisia leaf (Artemisia princeps Panpanini) (AFE) on the proliferation of endothelial cells, the cells from bovine aorta were cultured for up to 96 h in the presence of 1, 5, 10 or 50 micrograms/ml AFE in RPMI1640 medium supplemented with 10% fetal bovine serum...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaji T,Kaga K,Miezi N,Ejiri N,Sakuragawa N

更新日期：1990-02-01 00:00:00

abstract：:A new antibiotic indole trimer named trisindoline (1) was isolated, together with a known dioxopiperazine brevianamide F (2), from the culture of a bacterium of Vibrio sp., which was separated from the Okinawan marine sponge Hyrtios altum. The structure of trisindoline (1) has been determined on the bases of physicoch...

journal_title：Chemical & pharmaceutical bulletin

authors： Kobayashi M,Aoki S,Gato K,Matsunami K,Kurosu M,Kitagawa I

更新日期：1994-12-01 00:00:00

abstract：:A series of novel N6,N6-dialkyl adenosine 3',5'-cyclic phosphates N6,N6-dialkyl cAMPs) was synthesized from 2'-O-p-toluenesulfonyl cAMP (2'-O-tosyl cAMP, 2) and tested for inotropic and chronotropic activities in vitro. Treatment of 2 with excess alkyl halides and sodium hydride followed by detosylation with aqueous N...

journal_title：Chemical & pharmaceutical bulletin

authors： Kataoka S,Yamaji N,Kato M,Kawada T,Imai S

更新日期：1990-11-01 00:00:00

abstract：:N-Nitrosodialkylamines are alkylating carcinogens which are metabolically activated to alpha-hydroxy nitrosamines through oxidative dealkylation by cytochrome P450. In this study, the dealkylation step in the activation of N-nitrosodibenzylamine (NDBz) was investigated with metalloporphyrin/oxidant model systems under...

journal_title：Chemical & pharmaceutical bulletin

authors： Okochi E,Mochizuki M

更新日期：1995-12-01 00:00:00

abstract：:Two new naphthopyrones, cassiasides B2 (1) and C2 (2), were isolated from the seeds (Cassiae Semen) of Cassia obtusifolia L. The structures of the two new compounds 1 and 2 were established as rubrofusarin 6-O-beta-D- glucopyranosyl-(1-->6)-O-beta-D-glucopyranosyl-(1-->3)-O-beta-D- glucopyranosyl-(1-->6)-O-beta-D-gluc...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitanaka S,Nakayama T,Shibano T,Ohkoshi E,Takido M

更新日期：1998-10-01 00:00:00

abstract：:Certain amide-containing anthraquinone, xanthone, and carbazole derivatives have been synthesized and evaluated in vitro for their antiproliferative activities against a panel of human cancer cell lines including nasopharyngeal carcinoma (NPC-TW01), lung carcinoma (NCI-H661), and leukemia (Jurkat). Among them, 2-(9,10...

journal_title：Chemical & pharmaceutical bulletin

authors： Chen LC,Juang SH,Chang KM,Tzeng CC,Chen JJ,Chen IL,Wang TC

更新日期：2014-01-01 00:00:00

abstract：:A series of 2-alkylamino-5- or 6-aralkyl-substituted benzazoles were synthesized and tested for histamine H2-receptor antagonist and anti-stress ulcer activities. These new compounds showed little or no histamine H2-receptor antagonist activity in contrast to imidazo[1,2-a]pyridine analogues (I). On antiulcer assay, h...

journal_title：Chemical & pharmaceutical bulletin

authors： Katsura Y,Inoue Y,Tomoi M,Takasugi H

更新日期：1992-08-01 00:00:00

abstract：:The compound tentatively named TL-1 was isolated from Talaromyces luteus as a metabolite having monoamine oxidase (MAO) inhibitory potency. TL-1 showed mixed-type inhibition of MAO in mouse liver when kynuramine was used as a substrate, and the IC50 was 6.6 microM. The inhibition constants (Ki) for MAO-A and -B in mou...

journal_title：Chemical & pharmaceutical bulletin

authors： Satoh Y,Yamazaki M

更新日期：1989-01-01 00:00:00

abstract：:A series of 4-alkoxy-2-(1-piperazinyl)quinazoline derivatives was synthesized and evaluated for its ability to reverse a scopolamine-induced learned impairment in a one-trial passive avoidance task (antiamnestic activity). 2-(4-Allyl-1-piperazinyl)-4-pentyloxyquinazoline (4) showed more potent antiamnestic activity th...

journal_title：Chemical & pharmaceutical bulletin

authors： Hori M,Iemura R,Hara H,Sukamoto T,Ito K,Ohtaka H

更新日期：1991-02-01 00:00:00

abstract：:2-Acyl-tetrahydroisoquinoline-3-carboxylic acid derivatives were synthesized and biologically evaluated. (S)-2-(2,4-Hexadienoyl)-7-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (14) showed peroxisome proliferator-activated receptor γ (PPARγ) and PPARα agonist activities and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Otake K,Azukizawa S,Takahashi K,Fukui M,Shibabayashi M,Kamemoto H,Kasai M,Shirahase H

更新日期：2011-01-01 00:00:00

abstract：:An uncommon, previously unreported p-quinone-lignan compound called justicidone (4-(1,3-benzodioxol-5-yl)-6-methoxynaphtho[2,3-c]furan-1,5,8(3H)-trione) (2), along with the known savinin (1) were isolated from Justicia hyssopifolia (Acanthaceae). Their structures were determined by spectroscopic methods. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Andrés Pérez J,Boluda C,López H,Manuel Trujillo J

更新日期：2004-01-01 00:00:00

abstract：:Eight new guaipyridine sesquiterpene alkaloids, rupestines F-M (1-8) were isolated from the leaves of Artemisia rupestris and their structures were elucidated on the basis of 2D-NMR data. The absolute configurations of 1-8 have been assigned by comparison of their experimental and calculated circular dichroism (CD) sp...

journal_title：Chemical & pharmaceutical bulletin

authors： He F,Nugroho AE,Wong CP,Hirasawa Y,Shirota O,Morita H,Aisa HA

更新日期：2012-01-01 00:00:00

abstract：:Using tissue engineering technique to repair cartilage damage caused by osteoarthritis is a promising strategy. However, the regenerated tissue usually is fibrous cartilage, which has poor mechanical characteristics compared to hyaline cartilage. Chondrocyte hypertrophy plays an important role in this process. Thus, i...

journal_title：Chemical & pharmaceutical bulletin

authors： Cao Z,Dou C,Dong S

更新日期：2017-01-01 00:00:00

abstract：:We report a three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis of CDK2 inhibitors using fragment molecular orbital (FMO) calculations and partial least squares (PLS) regression. In our analysis, fragment binding energies of individual amino acids and fragment binding energy of a single l...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida T,Hirono S

更新日期：2019-01-01 00:00:00

abstract：:A series of 5-(4-aryl- or 4-arylcarbonylpiperazin-1-yl)-5-deoxy-1,4: 3,6-dianhydro-L-iditol 2-nitrates was prepared in order to obtain orally active, nitrate-type vasodilators with reduced side effects. Our drug design was based on a small reduction in the lipophilicity compared to that of 5-deoxy-5-[4-(3-phenylthiopr...

journal_title：Chemical & pharmaceutical bulletin

authors： Hayashi H,Ikeda J,Kubo K,Moriyama T,Karasawa A,Suzuki F

更新日期：1993-06-01 00:00:00

abstract：:Deacetylation of enynyl acetates under basic conditions allows convenient access to reactive allenyl ketones, which can then undergo 1,4-addition of nucleophiles to furnish β,γ-unsaturated ketones. Benzofuran and indole derivatives have also been obtained from enynyl acetates with an o-hetero-atom-substituted aryl gro...

journal_title：Chemical & pharmaceutical bulletin

authors： Okamoto N,Sueda T,Yanada R

更新日期：2016-01-01 00:00:00

abstract：:Evaluating the acute toxic effects of drugs or toxins is based mainly on studies which require the use of light microscopy. Recently, the effects of such substances on biological membranes, such as the nasal membrane, has been studied using the traditional Ussing chambers, which make it possible to study the transepit...

journal_title：Chemical & pharmaceutical bulletin

authors： Gizurarson S,Tamura S,Kurata T

更新日期：1991-06-01 00:00:00

abstract：:A series of novel disulfides containing 1,3,4-thiadiazole moiety were designed, synthesized, and the structures of all products were identified by spectral data (IR, NMR, and high resolution (HR)-MS). Their in vitro antiproliferative activities were evaluated using 2-(2-methoxy-4-nitro-phenyl)-3-(4-nitro-phenyl)-5-(2,...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang S,Liu XJ,Tang R,Wang HX,Liu HY,Liu YM,Chen BQ

更新日期：2017-01-01 00:00:00

abstract：:Separation of twelve sympathomimetic amines and related compounds by micellar electrokinetic chromatography (MEKC) with UV absorbance detection is described. These amines were well separated within 25 min using 50 mM sodium tetraborate solution containing 15 mM sodium dodecylsulfate (SDS) of pH 9.3 as a running soluti...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuroda N,Sato D,Ohyama K,Wada M,Nakahara Y,Nakashima K

更新日期：2001-07-01 00:00:00

abstract：:Debenzylating enzyme from Aspergillus niger enzyme (commercial crude cellulase) catalyzes the hydrolysis of cetraxate benzyl ester hydrochloride (2), a precursor of the antiulcer agent (1). The enzyme was highly purified by three kinds of chromatographies (hydrophobic, ion exchange, gel filtration) with a recovery of ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuroda H,Miyadera A,Imura A,Suzuki A

更新日期：1989-11-01 00:00:00

abstract：:Three cytotoxic cardenolides, acovenosigenin A 3-O-alpha-L-ramnopyranoside (1), euonymoside A (2) and euonymusoside A (3), were isolated from the woods of Euonymus alata (Celastraceae). The chemical structure of a new cardenolide, euonymusoside A (3) has been elucidated on the basis of extensive spectral analysis and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kitanaka S,Takido M,Mizoue K,Nakaike S

更新日期：1996-03-01 00:00:00