Chemical modification of fumagillin. II. 6-Amino-6-deoxyfumagillol and its derivatives.

abstract：:In the course of searching for selective growth inhibitors of the cancer cells adapted to nutrient starvation, a new 3-alkylpyridine alkaloid named N-methylniphatyne A (1) was isolated from an Indonesian marine sponge of Xestospongia sp. The chemical structure of 1 was determined on the basis of the spectroscopic anal...

journal_title：Chemical & pharmaceutical bulletin

authors： Arai M,Kamiya K,Shin D,Matsumoto H,Hisa T,Setiawan A,Kotoku N,Kobayashi M

更新日期：2016-01-01 00:00:00

abstract：:Tin(IV) complexes 2a--q derived from pyridine Schiff bases were prepared and characterized. Four complexes of this series were evaluated in vitro against different carcinogenic cell lines; besides their anti-inflammatory and antioxidant properties were also tested. Combination of mass spectrometry, multinuclear NMR an...

journal_title：Chemical & pharmaceutical bulletin

authors： González A,Gómez E,Cortés-Lozada A,Hernández S,Ramírez-Apan T,Nieto-Camacho A

更新日期：2009-01-01 00:00:00

abstract：:Enantiomerically pure (1S,3S)- and (1S,3R)-1-amino-3-(hydroxymethyl)cyclopentanes have been efficiently synthesized from L-aspartic acid. The title compounds are isosteres of ribose and may be used to construct nucleoside analogs with important antiviral and antineoplastic activities as demonstrated by a concise total...

journal_title：Chemical & pharmaceutical bulletin

authors： Rapoport H,Chen Y,Mohareb RM,Ahn JH,Sim TB,Ho JZ

更新日期：2003-10-01 00:00:00

abstract：:Each testosterone [125I]iodinated histamine derivative where [125I]iodinated histamines were linked to respective 15 alpha- and 15 beta-carboxymethyltestosterone (15 alpha- and 15 beta-CMT), testosterone-3-(O-carboxymethyl)oxime (T-3-CMO) and testosterone-17 beta-hemisuccinate (T-17-HS) were tested for their usefulnes...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyake Y,Shigetoshi M,Kojima M

更新日期：1990-04-01 00:00:00

abstract：:The effect of the surface layering time of lactose carrier particles on the dry powder inhalation properties of salbutamol sulfate was investigated. Lactose carrier particles were layered with vegetable magnesium stearate by physical mixing. In the present study, drug/carrier powder mixtures were designed consisting o...

journal_title：Chemical & pharmaceutical bulletin

authors： Iida K,Hayakawa Y,Okamoto H,Danjo K,Luenberger H

更新日期：2004-03-01 00:00:00

abstract：:Two sensitive and selective spectrofluorimetric and spectrophotometric stability-indicating methods have been developed for the determination of some non-steroidal anti-inflammatory oxicam derivatives namely lornoxicam (Lx), tenoxicam (Tx) and meloxicam (Mx) after their complete alkaline hydrolysis. The methods are ba...

journal_title：Chemical & pharmaceutical bulletin

authors： Taha EA,Salama NN,Fattah Lel-S

更新日期：2006-05-01 00:00:00

abstract：:A new class of mono and bis heterocycles-styrylsulfonylmethyl 1,3,4-oxadiazoles, pyrazolyl/isoxazolyl-1,3,4-oxadiazoles were prepared and studied their antioxidant activity. The compound methyl substituted 2-(p-methylphenylamino-sulfonylmethyl)-5-[Z-(p-methylstyrylsulfonylmethyl)]-1,3,4-oxadiazole displayed slightly h...

journal_title：Chemical & pharmaceutical bulletin

authors： Mallikarjuna Reddy G,Muralikrishna A,Padmavathi V,Padmaja A,Krishna Tilak T,Appa Rao C

更新日期：2013-01-01 00:00:00

abstract：:1,3-Dicapryloyl-2-linoleoylglycerol (1), a novel triglyceride, was isolated from berries of Hippophae rhamnoides. The structure was elucidated on the basis of MS, 1D and 2D NMR experiments including HMQC and HMBC. The metal chelating, free radical scavenging, and lipid peroxidation inhibiting properties of the compoun...

journal_title：Chemical & pharmaceutical bulletin

authors： Swaroop A,Sinha AK,Chawla R,Arora R,Sharma RK,Kumar JK

更新日期：2005-08-01 00:00:00

abstract：:The absorption of insulin (from porcine pancreas) from the rectum of rabbits after the administration of hollow-type suppositories containing insulin and five kinds of cyclodextrins (CyDs) was investigated. Three types of suppositories were employed: suppository I containing insulin (approximately 26 IU/mg) and variou...

journal_title：Chemical & pharmaceutical bulletin

authors： Watanabe Y,Matsumoto Y,Seki M,Takase M,Matsumoto M

更新日期：1992-11-01 00:00:00

abstract：:Based on the result of X-ray crystallographic analysis of our peroxisome proliferator-activated receptor alpha and delta (PPARalpha/delta) co-agonist complexed with human PPAR ligand binding domain (LBD), we designed and synthesized an optically active fluorescent PPARalpha/delta co-agonist, which has a pyrene unit in...

journal_title：Chemical & pharmaceutical bulletin

authors： Araya Y,Kasuga J,Toyota K,Hirakawa Y,Oyama T,Makishima M,Morikawa K,Hashimoto Y,Miyachi H

更新日期：2008-09-01 00:00:00

abstract：:Water-soluble porphyrins containing four platinum(II) complexes per molecule, [5alpha,10beta,15alpha,20beta-tetrakis(2-trans-(alpha,beta,alpha,beta-trans-Pt) and cis-(alpha,beta,alpha,beta-cis-Pt) [PtCl(NH(3))(2)]N-2-aminophenylporphyrin)], were synthesized and characterized. The binding of synthetic nucleotide polyme...

journal_title：Chemical & pharmaceutical bulletin

authors： Munakata H,Imai H,Nakagawa S,Osada A,Uemori Y

更新日期：2003-05-01 00:00:00

abstract：:A new resveratrol dimer and a new C-glucosyl resveratrol were isolated from stem wood of Hopea utilis along with nine stilbenoid derivatives comprising bergenin and (+)-lyoniresinol. The structures have been elucidated on the basis of the spectroscopic evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka T,Ito T,Ido Y,Nakaya K,Iinuma M,Chelladurai V

更新日期：2001-06-01 00:00:00

abstract：:In continuation of our efforts to discover novel nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs) as potentially "Safe NSAIDs," we report herein the design, synthesis and evaluation of 21 new NO-NSAIDs of commonly used NSAIDs such as aspirin, diclofenac, naproxen, flurbiprofen, ketoprofen, suli...

journal_title：Chemical & pharmaceutical bulletin

authors： Borhade N,Pathan AR,Halder S,Karwa M,Dhiman M,Pamidiboina V,Gund M,Deshattiwar JJ,Mali SV,Deshmukh NJ,Senthilkumar SP,Gaikwad P,Tipparam SG,Mudgal J,Dutta MC,Burhan AU,Thakre G,Sharma A,Deshpande S,Desai DC,Dubash

更新日期：2012-01-01 00:00:00

abstract：:Liposome uptake by HepG2 human hepatoma cells was investigated in comparison with the uptake by J774 murine macrophage-like cells. HepG2 cells accumulated liposomes (egg yolk phosphatidylcholine (EPC)/Chol; 75/25, diameter 0.2 micron) at 37 degrees C comparably to J774 macrophage-like cells. Confocal microscopic obser...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishiwata H,Sato SB,Kobayashi S,Oku M,Vertut-Doï A,Miyajima K

更新日期：1998-12-01 00:00:00

abstract：:New five seven-membered vibsane-type diterpenes named 5-epi-vibsanin C, 5-epi-vibsanin H, 5-epi-vibsanin K, 18-O-methyl-5-epi-vibsanin K and 5-epi-vibsanin E have been isolated from the leaves of Viburnum awabuki (Caplifoliaceae). Their structures have been elucidated by analyses of spectroscopic data and comparison o...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukuyama Y,Minami H,Matsuo A,Kitamura K,Akizuki M,Kubo M,Kodama M

更新日期：2002-03-01 00:00:00

abstract：:To expand the sequence of double-stranded DNA (dsDNA) targets in a triplex formation, 2',4'-BNAs (2'-O,4'-C-methylene bridged nucleic acids) having imidazoles as a nucleobase were synthesized and incorporated into oligonucleotides. Triplex-forming ability of the modified oligonucleotides was evaluated by using melting...

journal_title：Chemical & pharmaceutical bulletin

authors： Hari Y,Obika S,Inohara H,Ikejiri M,Une D,Imanishi T

更新日期：2005-07-01 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：:Prolyl endopeptidase (PEP, EC 3.4.21.26) is an enzyme playing a role in the metabolism of proline-containing neuropeptides which have been suggested to be involved in learning and memory processes. In screening for PEP inhibitors from fourteen traditional Kampo formulas, we found that Tokaku-joki-to shows a significan...

journal_title：Chemical & pharmaceutical bulletin

authors： Fan W,Tezuka Y,Kadota S

更新日期：2000-07-01 00:00:00

abstract：:To evaluate the usability of silk protein (sericin, SC) as a sustained-release material, the physicochemical properties of SC and the release profiles of model drugs from SC gel, sponge and film were studied. Heat aids the dissolution of SC. The molecular weight of SC tended to decrease as the heating temperature and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nishida A,Yamada M,Kanazawa T,Takashima Y,Ouchi K,Okada H

更新日期：2010-11-01 00:00:00

abstract：:Two new cangorosin A type triterpene dimers, which composed of two triterpene units jointed by two ether linkages between the A and B rings, were isolated from the Brazilian medicinal plant "xuxuá" (Maytenus chuchuhuasca). Structures of new isolates, xuxuasins A (1) and B (2), were established based on several spectro...

journal_title：Chemical & pharmaceutical bulletin

authors： Shirota O,Sekita S,Satake M,Morita H,Takeya K,Itokawa H

更新日期：2004-09-01 00:00:00

abstract：:Among the muscarinic acetylcholine receptor (mAChR) subtypes, the M4 receptor has been investigated as a promising drug target for the treatment of schizophrenia. These investigations have been based on findings from M4-deficient mice studies as well as on the results of a clinical trial that used xanomeline, an M1/M4...

journal_title：Chemical & pharmaceutical bulletin

authors： Takai K,Enomoto T

更新日期：2018-01-01 00:00:00

abstract：:We synthesize optically active (R)-terbutaline 2, which is an anti-asthmatic drug, through recyclable catalytic asymmetric transfer hydrogenation (RCATH). Various chloroketones 4 were prepared and RCATH was performed on them. The products exhibit moderate to high enantioselectivity. In particular, the hydrogenation of...

journal_title：Chemical & pharmaceutical bulletin

authors： Uchimoto H,Ikeda M,Tanida S,Ohhashi K,Chihara Y,Shigeta T,Arimitsu K,Yamashita M,Nishide K,Kawasaki I

更新日期：2017-01-01 00:00:00

abstract：:The bitter and sweet forms of a plant species differing with alkaloid contents may provide a model system for investigation of alkaloid biosynthesis at a molecular level. The pattern and concentration of quinolizidine alkaloids were determined by capillary GC-MS in bitter and sweet plants of Lupinus angustifolius. Bit...

journal_title：Chemical & pharmaceutical bulletin

authors： Hirai MY,Suzuki H,Yamazaki M,Saito K

更新日期：2000-10-01 00:00:00

abstract：:A new series of 3-(5-3-methyl-5-[(3-methyl-7-5-[2-(aryl)-4-oxo-1,3-thiazolan-3-yl]-1,3,4-thiadiazol-2-ylbenzo[b]furan-5-yl)methyl]benzo[b]furan-7-yl-1,3,4-thiadiazol-2-yl)-2-(aryl)-1,3-thiazolan-4-one 5a-j has been synthesized by the reaction of N2-[(E)-1-(4-methylphenyl)methylidene]-5-(3-methyl-5-[3-methyl-7-(5-[(E)-...

journal_title：Chemical & pharmaceutical bulletin

authors： Reddy CS,Rao DC,Yakub V,Nagaraj A

更新日期：2010-06-01 00:00:00

abstract：:Different crystal packing of hydrates from anhydrate crystals leads to different physical properties, such as solubility and stability. Investigation of the potential of varied hydrate formation, and understanding the stability in an anhydrous/hydrate system, are crucial to prevent an undesired transition during the m...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeuchi S,Kojima T,Hashimoto K,Saito B,Sumi H,Ishikawa T,Ikeda Y

更新日期：2015-01-01 00:00:00

abstract：:Transfer of aprindine from the blood into the intestinal lumen or into the peritoneal cavity was examined after intravenous administration of the drug at a dose of 5 mg/kg in rats. The amount of the drug transferred from the blood into the intestinal lumen was much greater than into the peritoneal cavity. The average ...

journal_title：Chemical & pharmaceutical bulletin

authors： Arimori K,Hashimoto Y,Nakano M

更新日期：1991-12-01 00:00:00

abstract：:A HPLC method for the simultaneous determination of 11 triterpene saponins with four-type aglycones (protopanaxadiol, protopanaxatriol, ocotillol and oleanolic acid types) in Ginseng drugs was developed and validated. Using a gradient of acetonitrile and 10 mM K-phosphate buffer (pH 5.80) as the mobile phase and UV de...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhu S,Zou K,Cai S,Meselhy MR,Komatsu K

更新日期：2004-08-01 00:00:00

abstract：:New alkenyl-1,4-benzoquinones, ardisianones A (1) and B (2), and the known maesanin (3) as 5-lipoxygenase inhibitors have been isolated from the rhizome of Ardisia japonica. Their structures have been elucidated as 2-methoxy-6-[(Z)-10'-pentadecenyl]-1,4-benzoquinone and 5-hydroxy-2-methoxy-6-[(Z)-8'-tridecenyl]-1,4-be...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukuyama Y,Kiriyama Y,Okino J,Kodama M,Iwaki H,Hosozawa S,Matsui K

更新日期：1993-03-01 00:00:00

abstract：:Binding sites of polyphenolic compounds on human serum albumin (HSA) were investigated using induced Cotton effects on the circular dichroism (CD) spectra. Polyphenolic compounds used in this study are known to be metabolites from tannins and their related polyphenols in food and medicinal plants. The present investig...

journal_title：Chemical & pharmaceutical bulletin

authors： Nozaki A,Kimura T,Ito H,Hatano T

更新日期：2009-09-01 00:00:00

abstract：:Chemical investigation on the stem of a Chinese mangrove plant Bruguiera sexangula var. rhynchopetala (Rhizophoraceae) resulted in the isolation and characterization of four new phenolic glycosides rhyncosides A-D (1-4), and two new lignan derivatives namely rhyncosides E-F (5-6), along with twelve known phenolic cons...

journal_title：Chemical & pharmaceutical bulletin

authors： Bao S,Ding Y,Deng Z,Proksch P,Lin W

更新日期：2007-08-01 00:00:00