A 3D-QSAR Analysis of CDK2 Inhibitors Using FMO Calculations and PLS Regression.

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：:The pH-dependence of the ability of coproporphyrin (CP) and uroporphyrin (UP) to photogenerate hydrogen peroxide (H2O2) in aqueous solution was investigated, with special attention to the structure-activity relationship related to the aggregation of the porphyrins. It was found that the efficiency was strongly depende...

journal_title：Chemical & pharmaceutical bulletin

authors： Komagoe K,Tamagake K,Katsu T

更新日期：2006-07-01 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：: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：:Freshwater cyanobacteria produce lethal toxins such as microcystins and anatoxins. During the purification of microcystins in bloom samples we found that a toxic cyanobacterium produced not only microcystins but also other types-peptides in early 1990. Since then we have isolated approximately thirty peptides from fre...

journal_title：Chemical & pharmaceutical bulletin

authors： Harada K

更新日期：2004-08-01 00:00:00

abstract：:Seven antioxidative serotonin derivatives were isolated from safflower (Carthamus tinctorius L.) oil cake. Their structures were established as N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]ferulamide (1), N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]-p-coumaramide (2), N,N'-[2,2'-(5,5'-dihydroxy-4,4'-bi-1H-indol-3,3'-yl)diethyl]- di-p-...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhang HL,Nagatsu A,Watanabe T,Sakakibara J,Okuyama H

更新日期：1997-12-01 00:00:00

abstract：:Two efficient and practical methods of synthesis of the C-10 substituent of DV-7751 (1), a novel quinolone carboxylic acid, were established. The first method utilizes an optical resolution of racemic 8-amino-6-benzyl-6-azaspiro[3.4]octane (13), while the second employs an enantioselective microbial reduction of 6-ben...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyadera A,Satoh K,Imura A

更新日期：2000-04-01 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：:Novel C(7)-derivatives of 1-cyclopropyl-6-fluoro-4-quinolone carboxylic acid (3a-o) have been synthesized and evaluated for in vitro antibacterial activity. Compounds 3e (3-aminocyclobutyl), 3g (1-aminocyclopropyl), 3m ((2-aminomethyl)vinyl), and 3o ((1-aminomethyl)vinyl) showed significant inhibitory activity, compar...

journal_title：Chemical & pharmaceutical bulletin

authors： Todo Y,Nitta J,Miyajima M,Fukuoka Y,Ikeda Y,Yamashiro Y,Saikawa I,Narita H

更新日期：1994-10-01 00:00:00

abstract：:An efficient stereocontrolled total synthesis of (+)-biotin (1) has been achieved via the intermediacy of Roche's lactone 5 starting from cis-1,3-dibenzyl-2-imidazole-4,5-dicarboxylic acid (2). The bifunctional cinchona alkaloid-derived squaramide-promoted enantioselective alcoholysis was utilizing as a tool for the c...

journal_title：Chemical & pharmaceutical bulletin

authors： Chen XX,Xiong F,Fu H,Liu ZQ,Chen FE

更新日期：2011-01-01 00:00:00

abstract：:New antitumor alkylglycerophospholipids, in which primarily the phosphocholine moiety of the platelet activating factor (PAF) molecule was modified, were synthesized from 1-alkyl-2-substituted glycerols by introducing polar head phosphoryl groups having methylene bridges of various lengths (from 2 to 14 carbons). They...

journal_title：Chemical & pharmaceutical bulletin

authors： Ukawa K,Imamiya E,Yamamoto H,Mizuno K,Tasaka A,Terashita Z,Okutani T,Nomura H,Kasukabe T,Hozumi M

更新日期：1989-05-01 00:00:00

abstract：:The purpose of this study was to determine which foods and/or drinks are capable of reducing the bitterness of topiramate when consumed together with the medicine. The inhibitory effects of foods/drinks (yoghurt and nine other foods/drinks) on the bitterness of topiramate (5 mg/mL) were evaluated with a taste sensor u...

journal_title：Chemical & pharmaceutical bulletin

authors： Haraguchi T,Uchida T,Hazekawa M,Yoshida M,Nakashima M,Sanda H,Hase T,Tomoda Y

更新日期：2016-01-01 00:00:00

abstract：:Four new bicyclic hexapeptides, named as RA-XI, -XII, XIII and -XIV were isolated from Rubia cordifolia and showed potent antitumor activities against P-388. The structures were elucidated from spectroscopic and chemical evidences. RA-XII, XIII and -XIV were proved to be unique bicyclic hexapeptidic glucosides. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Morita H,Yamamiya T,Takeya K,Itokawa H

更新日期：1992-05-01 00:00:00

abstract：:The biotransformation of 2α,5α,10β-triacetoxy-14-oxo-taxa-4(20),11-diene (1) by cultured Gingko cells afforded four products. Their structures were identified on the basis of analyses of the chemical and spectroscopic (IR, MS, ¹H- and ¹³C-NMR) data. Among them, 2, 3 and 5 were three new compounds, and 4 displayed pote...

journal_title：Chemical & pharmaceutical bulletin

authors： Xie D,Zhang Y,Zou J,Yin D,Chen X,Dai J

更新日期：2011-01-01 00:00:00

abstract：:Stomatitis induced by radiation therapy or cancer chemotherapy is a factor in sleep disorders and/or eating disorders, markedly decreasing patient quality of life. In recent years, disintegrating oral films that are easy to handle have been developed; therefore, we focused on the formulation of these films. We prepare...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawano Y,Sasatsu M,Mizutani A,Hirose K,Hanawa T,Onishi H

更新日期：2016-06-01 00:00:00

abstract：:Two monomethylated GM(3)-Type ganglioside molecular species, 1 and 2, have been obtained from the polar lipid fraction of the chloroform/methanol extract of the starfish Luidia maculata. The structures of these gangliosides have been determined on the basis of chemical and spectroscopic evidence as 1-O-[8-O-methyl-(N-...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawatake S,Inagaki M,Isobe R,Miyamoto T,Higuchi R

更新日期：2002-10-01 00:00:00

abstract：:Mutant activin receptor-like kinase-2 (ALK2) was reported to be closely associated with the pathogenesis of fibrodysplasia ossificans progressiva (FOP) and diffuse intrinsic pontine glioma (DIPG), and therefore presents an attractive target for therapeutic intervention. Through in silico virtual screenings and structu...

journal_title：Chemical & pharmaceutical bulletin

authors： Sekimata K,Sato T,Sakai N,Watanabe H,Mishima-Tsumagari C,Taguri T,Matsumoto T,Fujii Y,Handa N,Honma T,Tanaka A,Shirouzu M,Yokoyama S,Miyazono K,Hashizume Y,Koyama H

更新日期：2019-01-01 00:00:00

abstract：:The synthesis of acetomycin and related analogs was investigated. Acetomycin was synthesized from diethyl allyl(methyl)malonate in 6.5% yield over 18 steps. The total number of steps was improved compared to our previous synthesis; i.e., four steps shorter, and the total yield was 4.5% greater than the previous synthe...

journal_title：Chemical & pharmaceutical bulletin

authors： Uenishi J,Kobayashi N,Komine S,Okadai T,Yonemitsu O,Sasaki T,Yamada Y

更新日期：1999-04-01 00:00:00

abstract：:Novel potent regulators of tumor necrosis factor alpha (TNF-alpha) production by a human promyelocytic leukemia cell line, HL-60, were prepared. All the compounds showed inducer-specific and bidirectional regulation of TNF-alpha production, i.e., they enhanced 12-O-tetradecanoylphorbol-13-acetate-induced TNF-alpha pro...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyachi H,Azuma A,Hioki E,Kobayashi Y,Iwasaki S,Hashimoto Y

更新日期：1996-10-01 00:00:00

abstract：:Three new norlanostane-type triterpene glycosides, scillanostasides A, B, and C, and two new lanostane-type triterpene glycosides, scillanostasides D and E, were isolated from the bulbs of Scilla scilloides Druce (Liliaceae) along with one known norlanostane-type triterpene heptaglycoside, scillascilloside G-1. Their ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Toyohisa D,Morishita T,Horita H,Yasuda S,Nishida Y,Tanaka T,Okawa M,Kinjo J,Yoshimitsu H,Nohara T

更新日期：2011-01-01 00:00:00

abstract：:The purpose of this study was to predict the stability of octreotide in a mixed infusion containing sodium bisulfite (SBS). In aqueous solution the hydrolysis of octreotide was found to be accelerated by pH, and by increasing concentrations of SBS. Equations for the degradation rate constants (kobs) of pH and SBS were...

journal_title：Chemical & pharmaceutical bulletin

authors： Takasu Y,Yoshida M,Shimizu K,Asahara K,Tange M,Uchida T

更新日期：2014-01-01 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 series of 4-phenoxy-2-(1-piperazinyl)quinazolines was synthesized and examined for anticonvulsive and antihypoxic activities. Many of the compounds exhibited potent anticonvulsive activity comparable to that of carbamazepine or phenytoin. Among them, 4-phenoxy-2-(4-propyl-1-piperazinyl)quinazoline (5w) was selected ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hori M,Iemura R,Hara H,Ozaki A,Sukamoto T,Ohtaka H

更新日期：1990-03-01 00:00:00

abstract：:We investigated the distribution and stability of pirarubicin in human blood obtained from 12 healthy volunteers. The distribution of pirarubicin into blood cells showed marked temperature- and concentration-dependencies and the Arrhenius plot for pirarubicin uptake in blood was biphasic. Therefore, pirarubicin appear...

journal_title：Chemical & pharmaceutical bulletin

authors： Nagasawa K,Kitada N,Tsuji C,Ogawa M,Yokoyama T,Ohnishi N,Iwakawa S,Okumura K

更新日期：1992-10-01 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：:Polymorphic behaviours of paracetamol and propyphenazone and interaction between these two compounds were investigated using differential scanning calorimetry (DSC), X-ray powder diffraction and Fourier transform-infrared (FT-IR)-spectroscopy. Binary mixtures containing various ratios of the compounds were prepared as...

journal_title：Chemical & pharmaceutical bulletin

authors： Zalac S,Khan MZ,Gabelica V,Tudja M,Mestrović E,Romih M

更新日期：1999-03-01 00:00:00

abstract：:Aspartame (L-alpha-aspartyl-L-phenylalanine methyl ester) is a dipeptide sweetener about 200 times as sweet as sugar. It exists in crystal forms such as IA, IB, IIA, and IIB, which differ in crystal structure and in the degree of hydration. Among these, IIA is the most stable crystal form, and its crystal structure ha...

journal_title：Chemical & pharmaceutical bulletin

authors： Ebisawa K,Nagashima N,Fukuhara K,Kumon S,Kishimoto S,Suzuki E,Yoneda S,Umeyama H

更新日期：2000-05-01 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：:Sulfonic acid functionalized silica catalyzed the three-component reaction of aromatic amines, alpha,beta-unsaturated aldehydes and beta-keto esters forming the corresponding 1,4-dihydropyridines in short reaction times and in high yields. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Das B,Suneel K,Venkateswarlu K,Ravikanth B

更新日期：2008-03-01 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