Synthesis and cytostatic activity of 4,7-dihydroxythioaurone derivatives. Effect of B ring substitution on the activity.

abstract：:Glycyrrhetinic acid (Ia) and eighteen related derivatives were examined for antiulcer activity using stress-induced gastric lesions (restraint plus water immersion at 25 degrees C) in mice and rats as screening tests. Among the compounds tested, dihemiphthalate derivatives of 18 alpha- or 18 beta-olean-12-ene-3 beta,3...

journal_title：Chemical & pharmaceutical bulletin

authors： Yano S,Harada M,Watanabe K,Nakamaru K,Hatakeyama Y,Shibata S,Takahashi K,Mori T,Hirabayashi K,Takeda M

更新日期：1989-09-01 00:00:00

abstract：:Ginsenoside Rb1 is an important saponin of ginseng(s); however, Rb1, with 3-O- and 20-O-sugar moieties, has low bioavailability. Here, we report the derivatization of ginsenoside Rb1 to completely generate six types of highly bioactive minor ginsenoside Rg3 and its derivatives by FeCl3 catalysis, the reaction conditio...

journal_title：Chemical & pharmaceutical bulletin

authors： Yu H,Wang Y,Liu C,Yang J,Xu L,Li G,Song J,Jin F

更新日期：2018-01-01 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：:An efficient synthesis of the antiviral and antioxidative chromene (1) was achieved. A small amount of chromene 1 could be derived from plastoquinones 2 and 3, the major constituents of the brown alga, Sargassum micracanthum. By the following synthetic scheme involving its application, many kinds of analogs can be syn...

journal_title：Chemical & pharmaceutical bulletin

authors： Mori J,Iwashima M,Takeuchi M,Saito H

更新日期：2006-03-01 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：:In the course of an exploratory investigation of antitumor-promoting catechins, 3-O-acyl-(+)-catechins of varying carbon lengths from C(4) to C(18) were assessed for inhibitory effects on the activation of the Epstein-Barr virus early antigen. Like 3-O-acyl-(-)-epigallocatechins, the (+)-catechin derivatives showed pr...

journal_title：Chemical & pharmaceutical bulletin

authors： Uesato S,Taniuchi K,Kumagai A,Nagaoka Y,Seto R,Hara Y,Tokuda H,Nishino H

更新日期：2003-12-01 00:00:00

abstract：:Fibrinogen-related peptides, monomeric cyclic peptides through a disulfide bond [cyclo(H-Cys-Arg-Gly-Asp-Phe-Cys-NH2), cyclo(H-Cys-Arg-Gly-Asp-Phe-Cys-Gly-NH2), cyclo(H-Cys-Arg-Gly-Asp-Cys-NH2) and cyclo(H-Cys-Arg-Gly-Asp-Cys-Gly-NH2)], were prepared by the solid phase method with disulfide bond formation on the solid...

journal_title：Chemical & pharmaceutical bulletin

authors： Kakiuchi M,Izuno Y,Maeda M,Ueda K,Fujiwara K,Kunitada S,Kawasaki K

更新日期：1996-05-01 00:00:00

abstract：:Tumor necrosis factor related apoptosis-inducing ligand (TRAIL) has emerged as a promising anticancer agent as it selectively kills cancer cells. However, TRAIL resistance limits its use as a therapeutic agent. An understanding the mechanisms responsible for TRAIL resistance and strategies to overcome it are important...

journal_title：Chemical & pharmaceutical bulletin

authors： Ahmed F,Ishibashi M

更新日期：2016-01-01 00:00:00

abstract：:A high-performance liquid chromatographic method involving postcolumn fluorescence derivatization is described for the quantification of five fragment peptides (methionine-enkephalin-Thr-Ser-Glu-Lys, methionine-enkephalin-Lys, methionine-enkephalin-Arg, leucine-enkephalin-Lys and leucine-enkephalin-Arg) released by tr...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang GQ,Kai M,Ohkura Y

更新日期：1991-09-01 00:00:00

abstract：:Racemic 1-acetoxy-2-phenylpropane (12) and 1-acetoxy-2-(2-naphthyl)propane (33) were hydrolyzed with lipase at 35-36 degrees C for 2 and 24 h to give predominantly (S)-2-phenyl-1-propanol (11) and (S)-2-(2-naphthyl)-1-propanol (32), respectively. However, racemic 1-acetoxy-2-(1-naphthyl)propane (25) was recovered inta...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsumoto T,Takeda Y,Iwata E,Sakamoto M,Ishida T

更新日期：1994-06-01 00:00:00

abstract：:Allylamine (ALAM) film was plasma-polymerized on a flat glass (referred to as ALAM(GLA): GLA refers to a flat glass plate) for use as a solid phase in two-site immunoradiometric assay (two-site IRMA). Adsorption of F(ab')2 anti-human immunoglobulin G [formula: see text] to ALAM(GLA) was larger than adsorption on a pol...

journal_title：Chemical & pharmaceutical bulletin

authors： Muratsugu M,Kurosawa S,Mori Y,Kamo N

更新日期：1992-02-01 00:00:00

abstract：:alpha,alpha-Disubstituted amino acids are alpha-amino acids in which the hydrogen atom at the alpha-position of the L-alpha-amino acid is replaced with an alkyl substituent. The introduction of an alpha-alkyl substituent changes the properties of amino acids, with the conformational freedom of the side chain in the am...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka M

更新日期：2007-03-01 00:00:00

abstract：:The prediction of a protein three-dimensional (3D) structure is one of the most important challenges in computational structural biology. We have developed an automatic protein 3D structure prediction method called FAMSD. FAMSD is based on a comparative modeling method which consists of the following four steps: (1) g...

journal_title：Chemical & pharmaceutical bulletin

authors： Kanou K,Iwadate M,Hirata T,Terashi G,Umeyama H,Takeda-Shitaka M

更新日期：2009-12-01 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 beta-adrenoceptor-cyclic adenosine monophosphate (AMP) dependent glycogenolytic cascade was examined in normal rat hepatocytes and rat ascites hepatoma AH130 cells. The cyclic AMP content in AH130 cells was half of that in normal hepatocytes, and the cyclic AMP levels in both kinds of cells were clearly increased ...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyamoto K,Wakusawa S,Izumiya S,Koshiura R,Sakai R

更新日期：1990-02-01 00:00:00

abstract：:We prepared new antitumor active platinum complexes containing N,N'-bis(2-chloroethyl)ethylenediamine (ClEn) as an alkylating carrier ligand in order to obtain increased antitumor effects. Some of the platinum complexes synthesized showed enhanced antitumor activity. However, palladium(II) complexes containing ClEn we...

journal_title：Chemical & pharmaceutical bulletin

authors： Lee K,Tashiro T,Noji M

更新日期：1994-03-01 00:00:00

abstract：:Six new triterpenoid glycosides called julibrosides A1-A4, B1 and C1 were isolated from Albizziae Cortex, the dried stem bark of Albizzia julibrissin Durazz. Their structures were determined based on spectral and chemical evidence. Julibrosides B1 and C1 had new sapogenols, designated julibrogenin B and C, respectivel...

journal_title：Chemical & pharmaceutical bulletin

authors： Kinjo J,Araki K,Fukui K,Higuchi H,Ikeda T,Nohara T,Ida Y,Takemoto N,Miyakoshi M,Shoji J

更新日期：1992-12-01 00:00:00

abstract：:We developed a rapid and efficient analytical technique for cyclosporine A using HPLC on a column packed with 2-µm nonporous octadecylsilyl silica particles. Under optimized conditions, cyclosporine A was separated with high resolution from other cyclic peptides within 3 min, because the mass transfer resistance in th...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakai-Kato K,Nanjo K,Goda Y

更新日期：2018-01-01 00:00:00

abstract：:The stereoselective introduction of an allyl group into the angular position of 2-(TBS-oxymethyl)-2,3,4,6,7,8-hexahydro-1-benzopyran-5-one was accomplished using Birch reduction and an enolate trapping reaction. It was determined that the allyl group was introduced via an unexpected conformation-flipped from the initi...

journal_title：Chemical & pharmaceutical bulletin

authors： Hiroya K,Takahashi T,Shimomae K,Sakamoto T

更新日期：2005-02-01 00:00:00

abstract：:ZnAB has the combined structure of N,N-bis(2-pyridylmethyl)ethylenediamine as a specific chelater for Zn(2+) and 1,3,5,7-tetramethyl-8-phenyl-boron dipyrromethene as a fluorophore. Complexation of ZnAB with Zn(2+) produces a remarkable enhancement of fluorescence intensity. ZnAB has the advantages of less sensitivity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Koutaka H,Kosuge J,Fukasaku N,Hirano T,Kikuchi K,Urano Y,Kojima H,Nagano T

更新日期：2004-06-01 00:00:00

abstract：:Five glycyrrhetinic acid (Ib) derivatives have been synthesized to try to improve the antioxidant activity. Their in vitro antioxidant activities were studied using a cytochrome P450/NADPH reductase system from rat liver microsomes. The generation of microsomal free radicals was followed by oxidation of the DCFH-DA pr...

journal_title：Chemical & pharmaceutical bulletin

authors： Ablise M,Leininger-Muller B,Wong CD,Siest G,Loppinet V,Visvikis S

更新日期：2004-12-01 00:00:00

abstract：:Six new dammarane-type triterpene diglycosides with a hydroperoxide group, floralginsenosides A, B, C, D, E, and F, were isolated from ginseng flower, the flower buds of Panax ginseng C. A. MEYER, together with seven known dammarane-type triterpene oligoglycosides. The structures of new floralginsenosides were elucida...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa M,Sugimoto S,Nakamura S,Matsuda H

更新日期：2007-04-01 00:00:00

abstract：:The direct conversion of alpha-hydroxy ketones and alpha-keto oximes into quinoxaline derivatives in the presence of a catalytic amount of ceric ammonium nitrate via metal-catalyzed aerobic oxidation followed by in situ trapping with aromatic 1,2-diamines in water as a green and efficient reaction media, is reported. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Shaabani A,Maleki A

更新日期：2008-01-01 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：:Biodegradable pasty-type copolyesters with a relatively low molecular weight of 4500 were synthesized by direct copolycondensation of epsilon-caprolactone (CL) and delta-valerolactone (VL) in the absence of catalysts to evaluate in vivo capabilities of the polymer for implantable controlled release devices in drug del...

journal_title：Chemical & pharmaceutical bulletin

authors： Imasaka K,Yoshida M,Fukuzaki H,Asano M,Kumakura M,Mashimo T,Yamanaka H,Nagai T

更新日期：1991-08-01 00:00:00

abstract：:Further studies by means of preparative HPLC led to the isolation of two new furostanol saponins, macrostemonoside J (1) and L (3), along with an artifact, macrostemonoside K (2) from the bulbs of Allium macrostemon. On the basis of chemical evidence and spectral analysis (1H-, 13C-NMR and FAB-MS), the structure of 1 ...

journal_title：Chemical & pharmaceutical bulletin

authors： Peng J,Yao X,Okada Y,Okuyama T

更新日期：1994-10-01 00:00:00

abstract：:Four new bromotyrosine alkaloids, tyrokeradines C-F (1-4), have been isolated from Okinawan marine sponges of the order Verongidae. The structures of 1-4 were elucidated on the basis of spectroscopic data. Tyrokeradines C (1) and D (2) are new bromotyrosine alkaloids possesing an imidazole ring, while tyrokeradines E ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubota T,Watase S,Mukai H,Fromont J,Kobayashi J

更新日期：2012-01-01 00:00:00

abstract：:Three new natural sesquiterpene coumarins, isofeterin (1), lehmannolol (3), sinkianone (4), and one known compound, lehmannolone (2), were isolated from the roots of Ferula teterrima and Ferula sinkiangensis. Their chemical structures were established on the basis of spectroscopic analysis, including X-ray crystallogr...

journal_title：Chemical & pharmaceutical bulletin

authors： Yang JR,An Z,Li ZH,Jing S,Qina HL

更新日期：2006-11-01 00:00:00

abstract：:The analgesic components were isolated from a Bornean medicinal plant, Tabernaemontana pauciflora Blume (syn. Ervatamia blumeana Mark gr.), and the major components were identified as coronaridine and 3-(2-oxopropyl)coronaridine. Four minor components were estimated to be 5R- and 5S-(2-oxopropyl)coronaridine, 3-(2-oxo...

journal_title：Chemical & pharmaceutical bulletin

authors： Okuyama E,Gao LH,Yamazaki M

更新日期：1992-08-01 00:00:00

abstract：:(+)-4(5)-[(2R,5R)-5-aminomethyltetrahydrofuran-2-yl]imidazole [(+)-1, imifuramine] and its 2R,5S-stereoisomer (+)-2 were expected as base compounds to develop selective human histamine H4-receptor ligands. The improved synthesis of (+)-1 was done via cyclization of a diazafulvene intermediate generated by Bu3P/N,N,N',...

journal_title：Chemical & pharmaceutical bulletin

authors： Harusawa S,Araki L,Terashima H,Kawamura M,Takashima S,Sakamoto Y,Hashimoto T,Yamamoto Y,Yamatodani A,Kurihara T

更新日期：2003-07-01 00:00:00