Synthesis and cyclic AMP phosphodiesterase 4 isoenzyme inhibitory activity of heterocycle condensed purines.

abstract：:Polycomb repressive complex 2 (PRC2) is an attractive drug target for anti-cancer treatment. Among the three core subunits (EZH2, EED and SUZ12) of PRC2, EZH2 is the catalytic subunit that methylates histone H3 lysine 27 (H3K27), while EED is the regulatory subunit. Besides the small-molecule inhibitors of EZH2, those...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhu K,Du D,Yang R,Tao H,Zhang H

更新日期：2020-01-01 00:00:00

abstract：:To investigate the possible mechanism of the stimulatory effect of a hot water extract from Artemisia leaf (Artemisia princeps PANPANINI) (AFE) on the proliferation of endothelial cells, cells from bovine aorta were cultured for 72 h in RPMI1640 medium supplemented with 10% fetal calf serum in the presence of 5 microg...

journal_title：Chemical & pharmaceutical bulletin

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

更新日期：1990-09-01 00:00:00

abstract：:In our series of studies on potassium channel openers, several thienylcyanoguanidine derivatives were synthesized and evaluated for smooth muscle relaxation activity in vitro. Among the newly synthesized compounds, N-cyano-N'-(5-cyano-3-thienyl)-N"-tert-pentylguanidine (4b) and N-(5-bromo-3-thienyl)-N'-cyano-N"-tert-p...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshiizumi K,Ikeda S,Nishimura N,Yoshino K

更新日期：1997-12-01 00:00:00

abstract：:A convenient synthesis of immunosuppressive agent FTY720 (1) using the Petasis reaction was developed. 4-Octylbenzaldehyde (9) was converted into 1-ethenyl-4-octylbenzene (11) by two-step synthesis. Hydroboration of 11 using catecholborane and hydrolysis gave (E)-2-(4-octylphenyl)vinylboronic acid (4). The Petasis rea...

journal_title：Chemical & pharmaceutical bulletin

authors： Sugiyama S,Arai S,Kiriyama M,Ishii K

更新日期：2005-01-01 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：:Fe2+-dependent lipid peroxidation in phosphatidylcholine (PC) liposomes, assessed by thiobarbituric acid-reactive substances (TBARS) production, was stimulated in the presence of Fe3+ in a concentration-dependent manner. The rates of nitroblue tetrazolium (NBT) reduction and Fe2+ oxidation (Fe2+ disappearance and Fe3+...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohyashiki T,Kadoya A,Kushida K

更新日期：2002-02-01 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：:Indoloquinoline alkaloid cryptolepine and pyridocarbazole alkaloid ellipticine are of great interest because in vitro and in vivo studies revealed their good cytotoxic properties. In order to obtain some biologically active analogs of these compounds, we developed a synthesis based on the photocyclization of tertiary ...

journal_title：Chemical & pharmaceutical bulletin

authors： Aragon PJ,Yapi AD,Pinguet F,Chezal JM,Teulade JC,Blache Y

更新日期：2007-09-01 00:00:00

abstract：:Chemical investigations on the sea whip gorgonian coral Junceella juncea have led to the isolation of five new 8-hydroxybriarane diterpenoids, junceols D-H (1-5). The structures of briaranes 1-5 were determined on the basis of spectroscopic methods and the methylenecyclohexane rings were found to exist in boat form in...

journal_title：Chemical & pharmaceutical bulletin

authors： Sung PJ,Pai CH,Hwang TL,Fan TY,Su JH,Chen JJ,Fang LS,Wang WH,Sheu JH

更新日期：2008-09-01 00:00:00

abstract：:The title compounds, together with 3-vinylindolizine-1-carbonitriles (4-56%), were prepared in 1-18% yields from the S-alkylation of pyridinium 1-[3-ethoxycarbonyl-1-[cyanomethylthio(thiocarbonyl)]]all ylides with alkyl halides, followed by treatment of the resulting pyridinium salts with a base and then a dehydrogena...

journal_title：Chemical & pharmaceutical bulletin

authors： Kakehi A,Ito S,Hirata K,Zuo P

更新日期：2000-06-01 00:00:00

abstract：:(±)-8-Deisopropyladunctin B, the deisopropyl form of adunctin B, which was isolated from the leaves of Piper aduncum (Piperaceae) collected in Papua New Guinea, was synthesized in 0.77% overall yield in 17 steps from 5,7-dimethoxycoumarin-3-carboxylate. The key step was our original stereoconvergent skeleton transform...

journal_title：Chemical & pharmaceutical bulletin

authors： Nomura S,Arimitsu K,Yamaguchi S,Kosuga Y,Kakimoto Y,Komai T,Hasegawa K,Nakanishi A,Miyoshi T,Iwasaki H,Ozeki M,Kawasaki I,Kurume A,Ohta S,Yamashita M

更新日期：2012-01-01 00:00:00

abstract：:Squalene-2,3-epoxide: lanosterol cyclase was purified from rat liver in five steps as a soluble and homogeneous protein. The purified enzyme showed a single band on SDS-polyacrylamide gel electrophoresis with a molecular weight of 75 kD. In its native state it behaved as a homo-dimer. The isoelectric point of 5.5 and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kusano M,Abe I,Sankawa U,Ebizuka Y

更新日期：1991-01-01 00:00:00

abstract：:Fourteen new bisnor- and norditerpene dilactones, makilactones E-R, having a 7alpha : 8alpha-epoxy-9,11-enolide substructure, were isolated from a methanolic extract of the root and the bark of Podocarpus macrophyllus D. DON (Podocarpaceae) with thirteen known bisnor- and norditerpenoids, and the structures of those n...

journal_title：Chemical & pharmaceutical bulletin

authors： Sato K,Inaba Y,Park HS,Akiyama T,Koyama T,Fukaya H,Aoyagi Y,Takeya K

更新日期：2009-07-01 00:00:00

abstract：:We recently proposed a new hydrogen-accepting parameter, S(HA), for monosubstituted (di)azines on the basis of the heat of formation calculated by the conductor-like screening model (COSMO) method. In this work, S(HA) values for monosubstituted thiophenes and furans were calculated and the results were applied to the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamagami C,Tachikawa H

更新日期：2003-10-01 00:00:00

abstract：:We describe here a Tf₂NH-catalyzed formal (3+3) cycloaddition of silyl enol ethers with acrylates as a new domino reaction. In the domino sequence, the catalyst activates Michael addition, deprotonation of the resulting silyloxonium cation and intramolecular Claisen condensation. It was found that reaction modes signi...

journal_title：Chemical & pharmaceutical bulletin

authors： Azuma T,Takemoto Y,Takasu K

更新日期：2011-01-01 00:00:00

abstract：:Pyrrole-2,5-dicarboxylates were rapidly and selectively reduced to the corresponding mono-alcohol using 3 eq of diisobutylaluminum hydride at 0°C. Pyrrole-2,4-dicarboxylate showed the same reactivity; however, the selectivity decreased with pyrrole-3,4-dicarboxylate. When the nitrogen atom of the pyrrole-2,5-dicarboxy...

journal_title：Chemical & pharmaceutical bulletin

authors： Yasui E,Tsuda J,Ohnuki S,Nagumo S

更新日期：2016-01-01 00:00:00

abstract：:Manufacturing the solid dosage form of an orally administered drug requires lubrication to enhance manufacturability, ensuring that critical quality attributes such as disintegration and dissolution of the drug product are maintained during manufacture. Here, to evaluate lubrication performance during manufacture, we ...

journal_title：Chemical & pharmaceutical bulletin

authors： Dohi M,Momose W,Yamashita K,Hakomori T,Sato S,Noguchi S,Terada K

更新日期：2017-02-01 00:00:00

abstract：:A series of joro spider toxins, novel polyamines sharing a common moiety of 2,4-dihydroxyphenylacetyl cadaverine, have been identified using various bioassays, such as inhibition of a glutamatergic transmission and insecticidal activity. In this paper, we tried to chemically find still unknown polyamine toxins in the ...

journal_title：Chemical & pharmaceutical bulletin

authors： Chiba T,Akizawa T,Matsukawa M,Pan-Hou H,Yoshioka M

更新日期：1994-09-01 00:00:00

abstract：:Novel 1,2,3,4-tetrahydroisoquinoline derivatives bearing directly a cyclic amine at the 2-position were prepared and examined for their bradycardic activities in isolated right atria and in anesthetized rats. The structure-activity relationships (SAR) study revealed that the 2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinol...

journal_title：Chemical & pharmaceutical bulletin

authors： Kakefuda A,Watanabe T,Taguchi Y,Masuda N,Tanaka A,Yanagisawa I

更新日期：2003-04-01 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：: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：: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：:A 2,2'-[2,3-naphthylenebis(oxy)]-bis(N,N-diisopropyl(acetamide)) ligand (L) and its Gd(III) complex have been prepared and characterized. The crystal and molecular structure of the complex was determined by single-crystal X-ray diffraction. The interactions of complex with calf thymus DNA were investigated by UV-vis, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Lei K,Liu W,Huang X,Wang D

更新日期：2006-08-01 00:00:00

abstract：:Three new phenolic glycosides, named oplopanphesides A-C (1-3), have been isolated from the root barks of Oplopanax horridus. Their structures were elucidated by a combination of spectroscopic analyses, including 1D- and 2D-NMR techniques. These phenolic glycosides possess a novel feature in their sugar moieties that ...

journal_title：Chemical & pharmaceutical bulletin

authors： Huang WH,Zhang QW,Meng LZ,Yuan CS,Wang CZ,Li SP

更新日期：2011-01-01 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：:Several microorganisms showed the ability to transform the harman alkaloids, harmaline (1), harmalol (2) and harman (5). Harmaline (1) and harmalol (2) were converted by Rhodotorula rubra ATCC 20129 into the tryptamines, 2-acetyl-3-(2-acetamidoethyl)-7-methoxyindole (3) and 2-acetyl-3-(2-acetamidoethyl)-7-hydroxyindol...

journal_title：Chemical & pharmaceutical bulletin

authors： Herath W,Mikell JR,Ferreira D,Khan IA

更新日期：2003-06-01 00:00:00

abstract：:6-Amino-6-deoxyfumagillol (5) was synthesized by reductive amination of 6-oxo-6-deoxyfumagillol (4), which was obtained by oxidation of fumagillol (2). The reduction proceeded stereoselectively by the equatorial attack of hydride and 5 was found to have the same stereochemistry as that of 2. Several derivatives of 5 w...

journal_title：Chemical & pharmaceutical bulletin

authors： Marui S,Kishimoto S

更新日期：1992-03-01 00:00:00

abstract：:The aqueous ethanolic extract from the fresh stems of Opuntia dillenii HAW. showed potent radical scanvenging activity. Three new compounds, opuntioside I, 4-ethoxyl-6-hydroxymethyl-alpha-pyrone, and kaempferol 7-O-beta-D-glucopyranosyl-(1-->4)-beta-D-glucopyranoside, were isolated from the extract. The structures of ...

journal_title：Chemical & pharmaceutical bulletin

authors： Qiu Y,Chen Y,Pei Y,Matsuda H,Yoshikawa M

更新日期：2002-11-01 00:00:00

abstract：:Three new steroidal glycosides, named solaviasides A, B, and C, have been isolated from the fruits of Solanum viarum DUNAL (syn. S. khasianum var. chatterjeeanum, Solanaceae), along with seven known ones. Their chemical structures were determined on the basis of spectroscopic data and chemical evidence. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Kakiuchi T,Ebisawa H,Shiono Y,Nakamura T,Kai T,Ikeda T,Miyashita H,Yoshimitsu H,Nohara T

更新日期：2009-06-01 00:00:00

abstract：:From the ethyl acetate fraction of the stem bark of Camellia japonica, three new triterpenoids, 3beta-O-acetyl-16beta-hydroxy-12-oxoolean (6), 3beta-O-acetyl-16beta-hydroxy-11-oxoolean-12-ene (7), and 3beta-O-acetyl-16beta-hydroxyolean-12-ene (8), along with seven known compounds, 3alpha-hydroxy-1-oxofriedelan (1), fr...

journal_title：Chemical & pharmaceutical bulletin

authors： Thao NT,Hung TM,Lee MK,Kim JC,Min BS,Bae K

更新日期：2010-01-01 00:00:00