Design, Synthesis and Antiproliferative Evaluation of Novel Disulfides Containing 1,3,4-Thiadiazole Moiety.

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：:Microcrystalline cellulose (MCC) granules were prepared by wet granulation using a high-shear mixer. Physical characteristics of the granules were investigated using near IR spectrometry, thermogravimetry and isothermal water vapor adsorption. Near IR spectra of dried MCC granules prepared for various granulation time...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki T,Kikuchi H,Yonemochi E,Terada K,Yamamoto K

更新日期：2001-04-01 00:00:00

abstract：:Treatment composed of a gastric mucoadhesive antibiotic with slow release drug delivery is expected to be effective for the eradication of Helicobacter pylori (H. pylori). In this study, we evaluated the slow release property of the tetracycline-sucralfate acidic complex. Tetracycline was the antibiotic selected becau...

journal_title：Chemical & pharmaceutical bulletin

authors： Higo S,Takeuchi H,Yamamoto H,Hino T,Kawashima Y

更新日期：2008-10-01 00:00:00

abstract：:The amount of adsorption of bovine serum albumin (BSA) by hydroxyapatite (HAP) increased with a concentration of CaCl2 due to the bridging effect of Ca2+ between adsorbate BSA and adsorbent HAP. On the other hand, it decreased remarkably with a concentration of K2HPO4. This was explained in terms of the effects of ion...

journal_title：Chemical & pharmaceutical bulletin

authors： Shimabayashi S,Tanizawa Y,Ishida K

更新日期：1991-09-01 00:00:00

abstract：:A new C(19)-diterpenoid alkaloid, ouvrardiantine (1) and two new C(20)-diterpenoid alkaloids, ouvrardiandines A (2) and B (3) were isolated from the root of Aconitum ouvrardianum HAND.-MAZZ. The structure of the new alkaloids was established on the basis of spectral data (1D- and 2D-NMR, HR-MS). ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hou LH,Chen DL,Jian XX,Wang FP

更新日期：2007-07-01 00:00:00

abstract：:Targeted protein degradation by small molecules is an emerging modality with significant potential for drug discovery. We previously developed chimeric molecules, termed specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs), which induce the ubiquitylation and proteasomal de...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohoka N,Ujikawa O,Shimokawa K,Sameshima T,Shibata N,Hattori T,Nara H,Cho N,Naito M

更新日期：2019-03-01 00:00:00

abstract：:Thioglycosides are available donors in glycosylation due to the stability of the anomeric C-S bond under general reaction conditions of protection and deprotection, and offer orthogonality in their activation. We report now that the hypervalent iodine effectively induced glycosylation reaction of thioglycosides with v...

journal_title：Chemical & pharmaceutical bulletin

authors： Kajimoto T,Morimoto K,Ogawa R,Dohi T,Kita Y

更新日期：2016-01-01 00:00:00

abstract：:Mycobacterial cell walls have diverse adjuvant activities, and in particular, cell wall skeleton (CWS) of Mycobacterium bovis BCG has been expected as a drug for tumor immunotherapy. However, its molecular structure-biological activity relationship has not been fully elucidated despite more than 30 years of intensive ...

journal_title：Chemical & pharmaceutical bulletin

authors： Uenishi Y,Okada T,Okabe S,Sunagawa M

更新日期：2007-06-01 00:00:00

abstract：:We studied the possibility of using ursodeoxycholic acid (UDCA) as an excipient to create an amorphous composite that can be administered to animals in preclinical studies of experimental drugs. Three UDCA-based amorphous samples composed of nifedipine (NIF), indomethacin (IND), and naproxen (NAP) were found by screen...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanida S,Yoshimoto A,Yoshida M,Uchiyama H,Kadota K,Tozuka Y

更新日期：2019-01-01 00:00:00

abstract：:A series of 4-aza-5 alpha-androstane compounds with one or two aromatic moieties in the carbamoyl group at the C-17 position were synthesized and their inhibitory activities for rat and human prostatic testosterone 5 alpha-reductase were tested in vitro. Compounds with one aromatic moiety in the carbamoyl group showed...

journal_title：Chemical & pharmaceutical bulletin

authors： Kurata H,Ishibashi K,Saito S,Hamada T,Horikoshi H,Furukawa Y,Kojima K

更新日期：1996-01-01 00:00:00

abstract：:We have improved sample pre-treatment for the effective removal of polyphenols and simple analysis of caffeine in tea using a cartridge filled with polyvinylpolypyrroridone (PVPP). Nearly 100% of catechins were removed from the green tea sample and caffeine was completely recovered in the range of 98.2-101.3% by sampl...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamauchi Y,Nakamura A,Kitai M,Hatanaka K,Kohno I,Tanimoto T

更新日期：2007-09-01 00:00:00

abstract：:The disintegration kinetics of egg phosphatidylcholine small unilamellar liposomes in various bile salts (nine species) were investigated by monitoring turbidity changes with a stopped-flow apparatus. The pseudo-first-order rate constants obtained as a function of bile salt concentration (up to 25 mM) were analyzed ba...

journal_title：Chemical & pharmaceutical bulletin

authors： Nagata M,Yotsuyanagi T,Ikeda K

更新日期：1990-05-01 00:00:00

abstract：:Four new lignans, 3',4'-O,O-demethylenehinokinin (1), chamalignolide (2), 8'beta-hydroxyhinokinin (3) and 7beta,8beta-epoxyzuonin A (4), as well as (-)-hinokinin (5), and (-)-zuonin A (6), were isolated from the heartwood of Chamaecyparis obtusa var. formosana. The structures of these lignans were unambiguously determ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuo YH,Chen CH,Lin YL

更新日期：2002-07-01 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：: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：: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：:Four new lanostane triterpene lactones (colossolactone I, colossolactone II, colossolactone III and colossolactone IV) were isolated from the Vietnamese mushroom Ganoderma colossum (FR.) C. F. BAKER along with five known compounds. The structures of the new compounds were determined on the basis of MS, NMR and circula...

journal_title：Chemical & pharmaceutical bulletin

authors： El Dine RS,El Halawany AM,Nakamura N,Ma CM,Hattori M

更新日期：2008-05-01 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：:A series of diarylureas and diarylamides possessing pyrrolo[2,3-d]pyrimidine scaffold was designed and synthesized. The in vitro antiproliferative activities of a selected group of the target compounds against NCI-60 cell line panel were tested and compared with Sorafenib and Imatinib as reference compounds. Most of t...

journal_title：Chemical & pharmaceutical bulletin

authors： El-Gamal MI,Oh CH

更新日期：2014-01-01 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：:Regioselectivity in N-acetylation of nitro-0-phenylenediamine, a widely used hair dye component, by rat liver cytosolic N-acetyltransferases was studied in relation to its substituent effects on enzymatic N-acetylation of mono-substituted anilines. Nitro-p-phenylenediamine was acetylated specifically at the N4-positio...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakao M,Goto Y,Matsuki Y,Hiratsuka A,Watabe T

更新日期：1990-09-01 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：:Using CPG support linked with 5-deazaflavin, the 5-deazaflavin modified oligodeoxynucleotides at 3'-end(ODN-dF1) were synthesized. The thermal stability of the duplex of ODN-dF1 with its complement was higher than that of oligonucleotide linked to 5-deazaflavin at 5'-end internucleotide linkage. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakamura Y,Akiyama T,Bessho K,Yoneda F

更新日期：1993-07-01 00:00:00

abstract：:A series of dibenzofurans were efficiently and conveniently synthesized via one-pot consecutive C(sp(2))-O bond formation reaction (SNAr) in the presence of anhydrous K(2)CO(3), followed by C(sp(2))-C(sp(2)) bond formation reaction (intramolecular palladium-catalyzed aryl-aryl coupling reaction) between aryl halides a...

journal_title：Chemical & pharmaceutical bulletin

authors： Xu H,Fan LL

更新日期：2008-10-01 00:00:00

abstract：:The interaction of halofantrine with phosphatidylcholine and phosphatidylethanolamine bilayers has been investigated by differential scanning calorimetry. Halofantrine caused a broadening of the gel to liquid crystalline phase transition endotherm of the phosphatidylcholines. A decrease in the transition temperature T...

journal_title：Chemical & pharmaceutical bulletin

authors： Lim LY,Go ML

更新日期：1999-06-01 00:00:00

abstract：:Certain amide-containing anthraquinone, xanthone, and carbazole derivatives have been synthesized and evaluated in vitro for their antiproliferative activities against a panel of human cancer cell lines including nasopharyngeal carcinoma (NPC-TW01), lung carcinoma (NCI-H661), and leukemia (Jurkat). Among them, 2-(9,10...

journal_title：Chemical & pharmaceutical bulletin

authors： Chen LC,Juang SH,Chang KM,Tzeng CC,Chen JJ,Chen IL,Wang TC

更新日期：2014-01-01 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：:2-Acyl-tetrahydroisoquinoline-3-carboxylic acid derivatives were synthesized and biologically evaluated. (S)-2-(2,4-Hexadienoyl)-7-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (14) showed peroxisome proliferator-activated receptor γ (PPARγ) and PPARα agonist activities and ...

journal_title：Chemical & pharmaceutical bulletin

authors： Otake K,Azukizawa S,Takahashi K,Fukui M,Shibabayashi M,Kamemoto H,Kasai M,Shirahase H

更新日期：2011-01-01 00:00:00

abstract：:Of 4-amino-5-chloro-2-methoxy-N-(1-ethyl-2-hydroxymethyl-4- pyrrolidinyl)benzamide, four optical isomers, (2S,4S)-1 (TKS159), (2S,4R)-25, (2R,4S)-26 and (2R,4R)-27, were prepared from optically active 4-amino-1-ethyl-2-hydroxymethylpyrrolidine di-p-toluenesulfonate [(2S,4S)-14, (2S,4R)-17, (2R,4S)-20 and (2R,4R)-23, r...

journal_title：Chemical & pharmaceutical bulletin

authors： Yanagi T,Kitajima A,Anzai K,Kodama K,Mizoguchi J,Fujiwara H,Sakiyama H,Kamoda O,Kamei C

更新日期：1999-11-01 00:00:00

abstract：:A new series of 11-substituted 6,11-dihydrodibenz[b,e]oxepin derivatives was synthesized and evaluated for antiallergic activity. Convenient methods for the preparation of sulfides from alcohols were developed. Structure-activity relationships are described. Compound 7, 11-[2-(dimethylamin)ethyl]thio-6,11-dihydrodiben...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohshima E,Kumazawa T,Takizawa H,Harakawa H,Sato H,Obase H,Oiji Y,Ishii A,Ishii H,Ohmori K

更新日期：1991-10-01 00:00:00