New antitumor bicyclic hexapeptides, RA-XI, -XII, -XIII and -XIV from Rubia cordifolia.

abstract：:The percutaneous (p.c.) absorption of clonazepam (CZP), an antiepileptic drug, was investigated in rabbits. CZP was efficiently absorbed from a gel ointment (0.5% CZP, 1g, 9 cm2) with Azone and therapeutic plasma concentrations were maintained for 27 h. The bioavailability of CZP from the gel ointment was 47.2 +/- 3.1...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogiso T,Ito Y,Iwaki M,Yamamoto Y

更新日期：1989-02-01 00:00:00

abstract：:Peptide mimics derived from the first extracellular loop of CCR5 bearing non-peptide spacers in place of Ala-Ala-Ala sequence in the peptide moiety were synthesized, and the effects of these compounds on the inhibition against HIV-1 were examined. Compound 2b having m-aminophenoxyacetic acid derivative as a non-peptid...

journal_title：Chemical & pharmaceutical bulletin

authors： Ikeda K,Ishii Y,Konishi K,Sato M,Tanaka K

更新日期：2004-12-01 00:00:00

abstract：:All-methylated isorugosin B was synthesized via two-step esterification between optically active valoneic acid and glucose derivatives. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Shioe K,Takeuchi Y,Harayama T,Abe H

更新日期：2010-03-01 00:00:00

abstract：:Two new flavonoid glycosides, 5-hydroxy-7,8-dimethoxy (2R)-flavanone-5-O-beta-D-glucopyranoside (1) and 5-hydroxy-7,8,2',5'-tetramethoxy-flavone-5-O-beta-D-glucopyranoside (2), and a new diterpenoid, andrographic acid (3), along with andrographidine A (4) were isolated from Andrographis paniculata, and their structure...

journal_title：Chemical & pharmaceutical bulletin

authors： Li W,Xu X,Zhang H,Ma C,Fong H,van Breemen R,Fitzloff J

更新日期：2007-03-01 00:00:00

abstract：:Novel nucleoside analogues of structure 3-5 were synthesized starting from (+/-)-cis-2-amino-3-cyclopentenylmethanol (1). The chlorine derivative 3 inhibited both HIV-1 and HIV-2 replication in MT-4 cells with IC(50) values of 10.67 microM and of 13.79 microM, respectively. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Canoa P,González-Moa MJ,Teijeira M,Terán C,Uriarte E,Pannecouque C,De Clercq E

更新日期：2006-10-01 00:00:00

abstract：:Various novel methotrexate (MTX) derivatives bearing an indoline moiety were synthesized and tested for biological activities using human peripheral blood mononuclear cell (hPBMC) and human synovial cells (hSC) derived from patients with rheumatoid arthritis (RA). Compounds having potent activity in vitro were further...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuoka H,Kato N,Tsuji K,Maruyama N,Suzuki H,Mihara M,Takeda Y,Yano K

更新日期：1996-07-01 00:00:00

abstract：:(+)-6-(2-Chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4, 5-tetrahydro-8H-pyrido[4',3':4,5]thieno[3,2-f]triazolo[4,3-a] [1,4]diazepine (E6123) is a very potent platelet-activating factor (PAF) receptor antagonist and shows potent anti-PAF activities at the microgram level in a variety of animal models. In ord...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazawa S,Okano K,Kawahara T,Machida Y,Yamatsu I

更新日期：1992-03-01 00:00:00

abstract：:Two sesterterpenes, deoxymanoalide (1) and deoxysecomanoalide (2), were isolated from the nudibranch Chromodoris willani collected in Okinawa and their structures determined on the basis of spectroscopic data and chemical conversions. The mollusk feeds on a sponge containing manoalide (3) and secomanoalide (4) and is ...

journal_title：Chemical & pharmaceutical bulletin

authors： Uddin MH,Otsuka M,Muroi T,Ono A,Hanif N,Matsuda S,Higa T,Tanaka J

更新日期：2009-08-01 00:00:00

abstract：:Colon-specific drug delivery systems (CDDS) can improve the bioavailability of drug through the oral route. A novel formulation for oral administration using pH-enzyme Di-dependent chitosan mcirospheres (MS) and 5-Fu as a model drug has been investigated for colon-specific drug delivery by the emulsification/chemical ...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhao XL,Li KX,Zhao XF,Pang DH,Chen DW

更新日期：2008-07-01 00:00:00

abstract：:Two new megastigmane glucosides, called excoecariosides A and B were isolated from the leaves of a medicinal Vietnamese plant, Excoecaria cochinchinensis LOUR. var. cochinchinensis (Euphorbiaceae) together with seven known compounds. Their structures were elucidated by spectroscopic analyses and chemical reactions inc...

journal_title：Chemical & pharmaceutical bulletin

authors： Giang PM,Son PT,Matsunami K,Otsuka H

更新日期：2005-12-01 00:00:00

abstract：:From the ethanolic extract of the aerial parts of Globularia davisiana, a new iridoid glycoside, davisioside (1), was isolated. Davisioside (1) comprises a rare iridoid aglycone structure with a saturated double bond between C-3 and C-4. Nine known iridoid glycosides, asperuloside (2), alpinoside (3), geniposide (4), ...

journal_title：Chemical & pharmaceutical bulletin

authors： Caliş I,Kirmizibekmez H,Taşdemir D,Ireland CM

更新日期：2002-05-01 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 one-pot conversion of allyl alcohols into selenochroman derivatives was achieved by treatment with a phenyl trimethylsilyl selenide (TMSSePh)-AIBr3 reagent system. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Abe H,Yamasaki A,Koshiba N,Takeuchi Y,Harayama T

更新日期：2001-09-01 00:00:00

abstract：:2-(5-Arylidene-4-oxo-3-phenyl-thiazolidin-2-ylidene)-3-oxo-propionitriles 4a-j were prepared via condensation of aromatic aldehydes with 4-thiazolidinones 3a,b. The latter was obtained via electrophilic attack of phenylisothiocyanate on 3-oxo-propionitriles 1a,b followed by reaction with chloroacetyl chloride under ba...

journal_title：Chemical & pharmaceutical bulletin

authors： Hanna MM,George RF

更新日期：2012-01-01 00:00:00

abstract：:Simple one-pot methods for preparation of 2-oxazolines have been developed using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride (DMT-MM). Treatment of a mixture of carboxylic acids and 2-haloethylammonium salts with DMT-MM in methanol followed by refluxing in the presence of KOH gives oxazolines. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Hioki K,Takechi Y,Kimura N,Tanaka H,Kunishima M

更新日期：2008-12-01 00:00:00

abstract：:We describe herein a manganese(IV) oxide-mediated oxidation of N-p-methoxyphenyl (PMP)-protected glycine derivatives for the synthesis of α-imino carboxylic acid derivatives. Using this methodology, utilization of unstable glyoxic acid derivatives was avoided. Furthermore, using this methodology we synthesized novel α...

journal_title：Chemical & pharmaceutical bulletin

authors： Inokuma T,Jichu T,Nishida K,Shigenaga A,Otaka A

更新日期：2017-01-01 00:00:00

abstract：:Recently, active pharmaceutical ingredients (APIs) have been dramatically expanding from low-molecular weight drugs to peptides, proteins, antibodies, genes, oligonucleotides, cells, and machines. Therefore to develop pharmaceutical technologies and drug delivery systems (DDS) for these APIs, advanced molecules and no...

journal_title：Chemical & pharmaceutical bulletin

authors： Higashi T

更新日期：2019-01-01 00:00:00

abstract：:Binding sites of polyphenolic compounds on human serum albumin (HSA) were investigated using induced Cotton effects on the circular dichroism (CD) spectra. Polyphenolic compounds used in this study are known to be metabolites from tannins and their related polyphenols in food and medicinal plants. The present investig...

journal_title：Chemical & pharmaceutical bulletin

authors： Nozaki A,Kimura T,Ito H,Hatano T

更新日期：2009-09-01 00:00:00

abstract：:The synthesis and biological evaluation of [2-Valine-A] insulin ([Val2-A]insulin) is reported. In this insulin, the isoleucine residue in position A2, invariant in the majority of mammalian insulins, is substituted by valine. The same substitution, along with four others, occurs naturally in the insulin produced by th...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohta N,Burke GT,Katsoyannis PG

更新日期：1989-03-01 00:00:00

abstract：:The effect of metal ions on transcription of the ada gene of Escherichia coli which is promoted by Ada protein in the presence of methylated deoxyribonucleic acid (DNA) was examined in a reconstituted system. Their effect on the O6-methylguanine-DNA methyltransferase (MGTase) activity of Ada protein was also examined....

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi K,Suzuki M,Sekiguchi M,Kawazoe Y

更新日期：1992-09-01 00:00:00

abstract：:Mitomycin C, an anti-neoplastic agent, was covalently attached to bovine serum albumin through various kinds of spacers such as glutaryl, succinyl, trans-aconityl, methylsuccinyl and the trimellityl group. The prior acylation of albumin not only prevented protein polymerization in the presence of carbodiimide, but als...

journal_title：Chemical & pharmaceutical bulletin

authors： Kaneo Y,Tanaka T,Iguchi S

更新日期：1990-09-01 00:00:00

abstract：:Four new prenylated bibenzyls, named aglaiabbrevins A-D (2, 4-6), were isolated from the leaves of Aglaia abbreviata, along with two known related analogues, 3,5-dihydroxy-2-[3,7-dimethyl-2(E),6-octadienyl]bibenzyl (7) and 3,5-dihydroxy-2-(3-methyl-2-butenyl)bibenzyl (8). The structures of the new compounds were eluci...

journal_title：Chemical & pharmaceutical bulletin

authors： Sun P,Jiang CS,Zhang Y,Liu AH,Liang TJ,Li J,Guo YW,Jiang JM,Mao SC,Wang B

更新日期：2017-01-01 00:00:00

abstract：:A rapid method for the separation and purification of uridine diphosphate-glucuronosyltransferases (GT) was developed with the use of chromatofocusing on a high-performance liquid chromatograph. GT isoenzymes solubilized from hepatic microsomes of Wistar rats were separated on a Mono P column, a pre-packed column for ...

journal_title：Chemical & pharmaceutical bulletin

authors： Takanashi H,Homma H,Matsui M

更新日期：1989-06-01 00:00:00

abstract：:The analysis of genotoxic impurities (GTIs) in active pharmaceutical ingredients (APIs) is a challenging task. The target detection limit (DL) in an API is typically around 1 ppm (1 µg/g API). Therefore, a sensitive and selective analytical method is required for their analysis. 4-Chloro-1-butanol, an alkylating agent...

journal_title：Chemical & pharmaceutical bulletin

authors： Harigaya K,Yamada H,Yaku K,Nishi H,Haginaka J

更新日期：2014-01-01 00:00:00

abstract：:Chemical investigation on the constituents of the cones of Cycas beddomei has resulted in the isolation of a new biflavonoid, 2,3-dihydro-4'''-O-methyl amentoflavone, along with 2,3,2'',3''-tetrahydro hinokiflavone, 2,3,2'',3''-tetrahydro amentoflavone, 2,3-dihydro amentoflavone. The last two compounds were not report...

journal_title：Chemical & pharmaceutical bulletin

authors： Das B,Mahender G,Koteswara Rao Y,Prabhakar A,Jagadeesh B

更新日期：2005-01-01 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：: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：:N-Terminal tripeptide analogs of fibrin alpha-chain were synthesized and their inhibitory effect on fibrinogen/thrombin clotting was examined. A new water-soluble active ester, 3-pyridinium ester, was used for the synthesis. Among the synthetic peptides, H-Gly-Pro-Arg-hexamethyleneimine exhibited the highest inhibitor...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawasaki K,Tsuji T,Hirase K,Miyano M,Imoto Y,Iwamoto M

更新日期：1991-03-01 00:00:00

abstract：:We synthesized some 4,4'- and 2,2'-dihydroxytriphenylmethane derivatives 3a--e and 4a--c by condensation of phenol 1 and aromatic aldehyde 2 in moderate to good yields (30--83%). Most of them showed significant antiviral activity against herpes simplex virus type 1 (anti-HSV-1 activity) in a plaque reduction assay. Th...

journal_title：Chemical & pharmaceutical bulletin

authors： Mibu N,Yokomizo K,Uyeda M,Sumoto K

更新日期：2005-09-01 00:00:00

abstract：:Transfer of aprindine from the blood into the intestinal lumen or into the peritoneal cavity was examined after intravenous administration of the drug at a dose of 5 mg/kg in rats. The amount of the drug transferred from the blood into the intestinal lumen was much greater than into the peritoneal cavity. The average ...

journal_title：Chemical & pharmaceutical bulletin

authors： Arimori K,Hashimoto Y,Nakano M

更新日期：1991-12-01 00:00:00