Three new ingol diterpenes from Euphorbia nivulia: evaluation of cytotoxic activity.

abstract：:Chemical examination of a Chinese soft coral Lobophytum pauciflorum resulted in the isolation of seven new biscembranoids, named lobophytones H-N (1-7). Their structures were determined by interpretation of 1D- and 2D-NMR (correlation spectroscopy (COSY), heteronuclear single quantum coherence (HSQC), heteronuclear mu...

journal_title：Chemical & pharmaceutical bulletin

authors： Yan P,Deng Z,van Ofwegen L,Proksch P,Lin W

更新日期：2010-12-01 00:00:00

abstract：:Acetohydroxy acid synthase (AHAS; EC 2.2.1.6, also referred to as acetolactate synthase, ALS) has been considered as an attractive target for the design of herbicides. In this work, an optimized pyrazole sulfonamide base scaffold was designed and introduced to derive novel potential AHAS inhibitors by introducing a py...

journal_title：Chemical & pharmaceutical bulletin

authors： Lv XH,Ren ZL,Liu H,Li HD,Li QS,Wang L,Zhang LS,Yao XK,Cao HQ

更新日期：2018-01-01 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：:Novel hybrid L-ascorbic acid (vitamin C) derivatives with other biologically active substances, 5-hydroxy-2-hydroxymethyl-beta-pyrone (kojic acid) and alpha-tocopherol (vitamin E), linked at the C-2 or C-3 hydroxyl group were synthesized, and their thermal stability and inhibitory effects on tyrosinase activity, activ...

journal_title：Chemical & pharmaceutical bulletin

authors： Morisaki K,Ozaki S

更新日期：1996-09-01 00:00:00

abstract：:Adriamycin linked to oxidized dextran (ADM-OXD) via Schiff's base formation was compared with free adriamycin with regard to antitumor activity, acute toxicity and plasma pharmacokinetics in rats following i.v. administration. ADM-OXD showed higher activity against Walker carcinosarcoma 256 than free adriamycin. On th...

journal_title：Chemical & pharmaceutical bulletin

authors： Ueda Y,Munechika K,Kikukawa A,Kanoh Y,Yamanouchi K,Yokoyama K

更新日期：1989-06-01 00:00:00

abstract：:A novel cytolytic factor, dolabellanin P, was purified to apparent homogeneity from the purple fluid of the sea hare, Dolabella auricularia. Purified dolabellanin P is a single polypeptide of 60 kDa. The amino acid composition and the N-terminus of the factor were also determined. This factor nonspecifically lysed all...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamazaki M,Tansho S,Kisugi J,Muramoto K,Kamiya H

更新日期：1989-08-01 00:00:00

abstract：:An aniline derivative which corresponds to UV-5 in the preceding paper was isolated from the case L-tryptophan sample associated with eosinophilia-myalgia syndrome (EMS). By spectroscopic analyses, the structure was identified as 3-anilinoalanine. The compound was optically active, and the stereochemistry of alanine m...

journal_title：Chemical & pharmaceutical bulletin

authors： Goda Y,Suzuki J,Maitani T,Yoshihira K,Takeda M,Uchiyama M

更新日期：1992-08-01 00:00:00

abstract：:Infection with Helicobacter pylori (H. pylori) plays an important role in the pathogenesis of gastritis, peptic ulcer and gastric cancer, and the 13C-urea breath test (13C-UBT) is a convenient and non-invasive method for the detection of H. pylori in the stomach. We have examined the sensitivity, specificity and accur...

journal_title：Chemical & pharmaceutical bulletin

authors： Kajiwara M,Iida K,Takatori K,Taniguchi Y,Kimura K

更新日期：1997-04-01 00:00:00

abstract：:This study examined the intestinal transport of five harman alkaloids using the Caco-2 cell monolayer as a model of the human intestinal mucosa. Transport parameters, permeability coefficients and percent transports, were calculated and compared under identical conditions with atenolol. Permeability coefficients were ...

journal_title：Chemical & pharmaceutical bulletin

authors： Khan SI,Abourashed EA,Khan IA,Walker LA

更新日期：2004-04-01 00:00:00

abstract：:A new series of highly potent angiotensin-converting enzyme (ACE) inhibitors, 1-(N2-substituted L-lysyl-gamma-D-glutamyl)octahydro-1H-indole-2-carboxylic acids, was synthesized; various acyl groups were introduced at the alpha-amino group of the N-terminal P1 Lys. The effect of the N2-acyl groups on in vitro inhibitor...

journal_title：Chemical & pharmaceutical bulletin

authors： Sawayama T,Tsukamoto M,Sasagawa T,Nishimura K,Deguchi T,Takeyama K,Hosoki K

更新日期：1990-01-01 00:00:00

abstract：:Chemical investigation of the seeds of Adonis aestivalis has led to the isolation of a new cardenolide (3β,5α,14β,17β-tetrahydroxycard-20,22-enolide) (1), two new glycosides (2, 3) of 1, and a new strophanthidin hexaglycoside (4), together with a known compound, strophanthidin 3-O-β-D-glucopyranoside (5). The structur...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubo S,Kuroda M,Matsuo Y,Masatani D,Sakagami H,Mimaki Y

更新日期：2012-01-01 00:00:00

abstract：:The microbial transformation of five flavans (1-5) by endophytic fungi isolated from the tea plant Camellia sinensis was investigated. It was found that the endophytic filamentous fungus Diaporthe sp. oxidized stereoselectively at C-4 position of (+)-catechin (1) and (-)-epicatechin (2) to give the correspondent 3,4-c...

journal_title：Chemical & pharmaceutical bulletin

authors： Agusta A,Maehara S,Ohashi K,Simanjuntak P,Shibuya H

更新日期：2005-12-01 00:00:00

abstract：:Four acyclic diterpene glycosides were extracted from Habanero, the fruits of Capsicum chinense JACQ., which is known as one of the hottest peppers in existence. Two of these glycosides were identified as capsianoside XIII and capsianoside XV. The other two were new ones and were characterized as 3-O-beta-D-glucopyran...

journal_title：Chemical & pharmaceutical bulletin

authors： Lee JH,El-Aasr M,Ikeda T,Oda K,Miyashita H,Yoshimitsu H,Okawa M,Kinjo J,Nohara T

更新日期：2009-07-01 00:00:00

abstract：:One novel sesquiterpene with new skeleton, (6S)-2-methyl-6-(4-hydroxyphenyl-3-methyl)-2-hepten-4-one (1), two new bisabolane sesquiterpenes, (6S)-2-methyl-6-(4-hydroxyphenyl)-2-hepten-4-one (2), (6S)-2-methyl-6-(4-formylphenyl)-2-hepten-4-one (3), and two calebin derivatives, 4''-(4'''-hydroxyphenyl-3'''-methoxy)-2''-...

journal_title：Chemical & pharmaceutical bulletin

authors： Zeng Y,Qiu F,Takahashi K,Liang J,Qu G,Yao X

更新日期：2007-06-01 00:00:00

abstract：:A series of substituted 6,7-dihydro-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acids was synthesized and tested for antibacterial activities. Among them, 9-fluoro-6,7-dihydro-5-methyl-8-(4-methyl-1-piperazinyl)-1-oxo-1H,5H- benzo[i,j]quinolizine-2-carboxylic acid (OPC-7241) exhibited potent antibacterial activity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishikawa H,Tabusa F,Miyamoto H,Kano M,Ueda H,Tamaoka H,Nakagawa K

更新日期：1989-08-01 00:00:00

abstract：:Bis[2-[(E)-2-octenoylamino]ethyl] disulfide (compd. I-3) inhibited collagen- and arachidonic acid-induced rat platelet aggregation, although not adenosine 5'-diphosphate (ADP)-induced rat platelet aggregation. Based on these results, we then investigated the inhibitory effect of compd. I-3 on thromboxane B2 formation ...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimura T,Nakajima H,Tsujikawa K,Yasuda N,Haruyama M,Okabe M,Iwai M,Yokoyama K

更新日期：1989-03-01 00:00:00

abstract：:A novel series of 2-acyl-3-carboxyl-tetrahydroisoquinoline derivatives were synthesized and biologically evaluated. Among them, (S)-2-{(E)-3-furan-2-ylacryloyl}-7-[(2E,4E)-5-(2,4,6-trifluorophenyl)penta-2,4-dienyloxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (compound 17u) was identified as a potent protein ty...

journal_title：Chemical & pharmaceutical bulletin

authors： Morishita K,Shoji Y,Fukui M,Ito Y,Kitao T,Ozawa SI,Hirono S,Shirahase H

更新日期：2018-01-01 00:00:00

abstract：:The effect of chromomycin A3 binding on the geometry of DNA duplex (plasmid pBR322) has been examined using topoisomerase I relaxation followed by gel electrophoresis. To determine the equilibrium constant of this drug-DNA binding-dissociation reaction in the same concentration range (ca. 10(-5) M) in the same buffer ...

journal_title：Chemical & pharmaceutical bulletin

authors： Utsuno K,Kojima K,Maeda Y,Tsuboi M

更新日期：1998-11-01 00:00:00

abstract：:N-9-Fluorenylmethoxycarbonyl-Se-4-methoxybenzylselenocysteine++ + [Fmoc-Sec(MBzl)-OH] was synthesized from selenocystine and successfully applied to Fmoc-based solid-phase peptide synthesis. The stability and the deprotection conditions of the Se-MBzl group were examined. The diselenide bond of a peptide was directly ...

journal_title：Chemical & pharmaceutical bulletin

authors： Koide T,Itoh H,Otaka A,Yasui H,Kuroda M,Esaki N,Soda K,Fujii N

更新日期：1993-03-01 00:00:00

abstract：:A highly sensitive spectrophotometric determination of human serum albumin (HSA) with 3',4',5',6'-tetrachlorogallein (T.Cl.Gall)-Mo(VI) complex in a Triton X-100 + polyvinyl alcohol micellar medium is proposed. This method can be used to determine up to ca. 150 micrograms/10 ml of HSA from the optical absorbance at 64...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujita Y,Mori I,Ikuta K,Nakahashi Y,Kato K,Nakanishi T

更新日期：1989-09-01 00:00:00

abstract：:Polyamines, especially spermine, inhibit N-methyl-D-aspartate (NMDA) receptors as open channel blockers. Two types of water-soluble NMDA receptor antagonist, ACCn (1) and TGCn (2), with a 1,4,7,10-tetraazacyclododecane cyclic polyamine group, were synthesized and the effects of both compounds on NMDA receptors were st...

journal_title：Chemical & pharmaceutical bulletin

authors： Masuko T,Metori K,Kizawa Y,Kusama T,Miyake M

更新日期：2005-04-01 00:00:00

abstract：:Novel 4,5,6,7-tetrahydrothieno[3,2-c]pyridines, 1-thienyl-1,2,3,4-tetrahydroisoquinolines and related compounds, in which the benzene rings of (+)-1 (FR115427) were replaced with heteroaromatic rings such as thiophene, furan, benzothiophene and indole, were synthesized and evaluated for anticonvulsant activity against...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohkubo M,Kuno A,Katsuta K,Ueda Y,Shirakawa K,Nakanishi H,Kinoshita T,Takasugi H

更新日期：1996-04-01 00:00:00

abstract：:Novel sialosyl donors, 4-pentenoic acid ester of N-acetylneuraminic acids (Neu5Ac) and 4-pentenyl glycoside of Neu5Ac were successfully prepared from the corresponding per-O-acetylated 2-hydroxy and 2-chloro derivatives of Neu5Ac, respectively and applied to the synthesis of O-sialosides. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikeda K,Fukuyo J,Sato K,Sato M

更新日期：2005-11-01 00:00:00

abstract：:Conferols A (1) and B (2), the new 4-hydroxyisoflavones, have been isolated from the dichloromethane sub-fraction of the methanolic extract of Caragana conferta along with 3',5'-dihydroxy, 7,4'-dimethoxyisoflavone (3), E-cinnamic acid (4), tetracosyl 3,4-dihydroxy-E-cinnamate (5), docosyl 3,4-dihydroxy-E-cinnamate (6)...

journal_title：Chemical & pharmaceutical bulletin

authors： Khan R,Malik A,Adhikari A,Qadir MI,Choudhary MI

更新日期：2009-04-01 00:00:00

abstract：:In continuing our program aimed to search for tyrosinase inhibitors, a series of novel 4-O-substituted phenylmethylenethiosemicarbazones were rational designed, synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were also evaluated. A fair number of compounds were found to have...

journal_title：Chemical & pharmaceutical bulletin

authors： Yi W,Cao R,Chen Z,Yu L,Wen H,Yan Q,Ma L,Song H

更新日期：2010-05-01 00:00:00

abstract：:Novel neutral glycosphingolipids isolated from the plerocercoids of a tapeworm, Spirometra erinacei, may be expected to be involved in host-parasite interactions. We have synthesized this glycosphingolipid analogue containing 2-branched fatty alkyl residue in place of ceramide. Glycosylation of nonreducing-end trisacc...

journal_title：Chemical & pharmaceutical bulletin

authors： Hada N,Kuroda M,Takeda T

更新日期：2000-08-01 00:00:00

abstract：:Biological activity of thioaurones was not tested so far and the group constitute completely unexplored source of new molecules of pharmacological interest. We report synthesis and evaluation of cytotoxic activity of thioaurone derivatives bearing p-hydroquinone system in ring A. Their activity was found to depend str...

journal_title：Chemical & pharmaceutical bulletin

authors： Konieczny MT,Konieczny W,Okabe S,Tsujimoto H,Suda Y,Wierzba K

更新日期：2006-03-01 00:00:00

abstract：:The oxidative behaviour of, a hypnotic drug, zolpidem was studied at glassy carbon electrode in Britton-Robinson buffer over the pH range 2.0-11.0 using cyclic, linear sweep and differential pulse voltammetry. Oxidation of the drug was effected in a single irreversible, diffusion-controlled step. Using differential pu...

journal_title：Chemical & pharmaceutical bulletin

authors： Radi AE,Bekhiet G,Wahdan T

更新日期：2004-09-01 00:00:00

abstract：:A series of novel 1-(6,7-dimethoxy-4-quinazolinyl)piperidines carrying substituted hydantoin and 2-thiohydantoin rings was synthesized and examined for cardiotonic activity in anesthetized dogs. Introduction of isopropyl and sec-butyl group at the 5-position of the hydantoin and thiohydantoin rings led to potent inotr...

journal_title：Chemical & pharmaceutical bulletin

authors： Nomoto Y,Takai H,Hirata T,Teranishi M,Ohno T,Kubo K

更新日期：1990-11-01 00:00:00

abstract：:The object of this study was to develop hydroxypropyl methylcellulose (HPMC) based cephalexin extended release tablet, which can release the drug for six hours in predetermined rate. Twenty-one batches of cephalexin tablets were prepared by changing various physical and chemical parameters, in order to get required th...

journal_title：Chemical & pharmaceutical bulletin

authors： Saravanan M,Sri Nataraj K,Ganesh KS

更新日期：2003-08-01 00:00:00