Development of a cyclosporin A derivative with excellent anti-hepatitis C virus potency.

abstract：:Platinum compounds are the first-line therapy for many types of cancer. However, drug resistance has frequently been reported for and is a major limitation of platinum-based chemotherapy in the clinic. In the current study, we examined the anti-tumor activity of phomoxanthone A (PXA), a tetrahydroxanthone dimer isolat...

journal_title：Bioorganic & medicinal chemistry

authors： Wang C,Engelke L,Bickel D,Hamacher A,Frank M,Proksch P,Gohlke H,Kassack MU

更新日期：2019-10-01 00:00:00

abstract：:Previous studies have shown that several imidazole derivatives possess affinity to histamine H(3) and H(4) receptors. Continuing our study on structural requirements responsible for affinity and selectivity for H(3)/H(4) receptor subtypes, two series of 3-(1H-imidazol-4-yl)propyl carbamates were prepared: a series of ...

journal_title：Bioorganic & medicinal chemistry

authors： Więcek M,Kottke T,Ligneau X,Schunack W,Seifert R,Stark H,Handzlik J,Kieć-Kononowicz K

更新日期：2011-05-01 00:00:00

abstract：:We examined the in vitro and in vivo natural killer (NK) cell activity enhancing effects of alpha-, beta-galactosylceramide (GalCer) and alpha-, beta-glucosylceramide (GluCer) which have the same ceramide moiety, and of other alpha-, beta-GalCer having a different ceramide portion, and found that alpha-types show stro...

journal_title：Bioorganic & medicinal chemistry

authors： Kobayashi E,Motoki K,Yamaguchi Y,Uchida T,Fukushima H,Koezuka Y

更新日期：1996-04-01 00:00:00

abstract：:Two types of structural variants of D-myo-inositol 1,4,5-trisphosphate [Ins(1,4,5)P3] were prepared by a chemoenzymatic route. These 6-O-substituted analogues retained the biological activity of Ins(1,4,5)P3, and were able to elicit Ca2+ release from porcine brain microsomes. Moreover, these derivatives allowed the pr...

journal_title：Bioorganic & medicinal chemistry

authors： Gou DM,Shieh WR,Lu PJ,Chen CS

更新日期：1994-01-01 00:00:00

abstract：:Both histone deacetylase (HDAC) and fibroblast growth factor receptor (FGFR) are important targets for cancer therapy. Although combining dual HDAC pharmacophore with tyrosine kinase inhibitors (TKIs) had achieved a successful progress, dual HDAC/FGFR1 inhibitors haven't been reported yet. Herein, we designed a series...

journal_title：Bioorganic & medicinal chemistry

authors： Liu J,Qian C,Zhu Y,Cai J,He Y,Li J,Wang T,Zhu H,Li Z,Li W,Hu L

更新日期：2018-02-01 00:00:00

abstract：:Due to the capability of peptidyl derivatives of araC to behave as prodrugs of this antimetabolite, and because of the well known biological properties of peptide T and its analogues (in particular that of targeting CD4+ cells), new peptide T-araC conjugates were prepared and tested in vitro for antiproliferative acti...

journal_title：Bioorganic & medicinal chemistry

authors： Manfredini S,Marastoni-M,Tomatis R,Durini E,Spisani S,Pani A,Marceddu T,Musiu C,Marongiu ME,La Colla P

更新日期：2000-03-01 00:00:00

abstract：:In our previous work, a series of 2-amino-3,4-dihydroquinazoline derivativesusing an electron acceptor group was reported to be potent T-type calcium channel blockers and exhibit strong cytotoxic effects against various cancerous cell lines. To investigate the role of the guanidine moiety in the 2-amino-3,4-dihydroqui...

journal_title：Bioorganic & medicinal chemistry

authors： Nam Y,Ryu KD,Jang C,Moon YH,Kim M,Ko D,Chung KS,Gandini MA,Lee KT,Zamponi GW,Lee JY

更新日期：2020-06-01 00:00:00

abstract：:The intestinal absorption of an intact oligopeptide was investigated in rats using a synthetic cationic peptide, 001-C8 (H-MeTyr-Arg-MeArg-D-Leu-NH(CH2)8NH2). The peptide was coupled with 4-nitrobenzo-2-oxa-1,3-diazole (NBD) to prepare a fluorescence-labeled derivative 001-C8-NBD (H-MeTyr-Arg-MeArg-D-Leu-NH(CH2)8NH-NB...

journal_title：Bioorganic & medicinal chemistry

authors： Sai Y,Kajita M,Tamai I,Kamata M,Wakama J,Wakamiya T,Tsuji A

更新日期：1998-06-01 00:00:00

abstract：:A series of novel metronidazole aryloxy, carboxy and azole derivatives has been synthesized and their cytotoxic activities on three cancer cell lines were evaluated by MTT assay. Compounds 4m, 4l and 4d showed the most potent cytotoxic activity (IC50s less than 100 µg/mL). Apoptosis was also detected for these compoun...

journal_title：Bioorganic & medicinal chemistry

authors： Faghih-Mirzaei E,Sabouri S,Zeidabadinejad L,AbdolahRamazani S,Abaszadeh M,Khodadadi A,Shamsadinipour M,Jafari M,Pirhadi S

更新日期：2019-01-15 00:00:00

abstract：:As part of our ongoing research on potential new antiepileptic drugs (AEDs), a series of tetramethylcyclopropanecarboxamide derivatives containing benzene ring were designed, synthesized, and evaluated for anticonvulsant activities in the murine maximal electroshock (MES) and subcutaneous pentylenetetrazole (scMet) se...

journal_title：Bioorganic & medicinal chemistry

authors： Shimshoni JA,Bialer M,Yagen B

更新日期：2008-06-01 00:00:00

abstract：:A series of 3-amino-benzo[d]isoxazole-/3-aminoindazole-based compounds were designed, synthesized and pharmacologically evaluated as tyrosine kinase c-Met inhibitors. The SAR study was conducted leading to identification of nine compounds (8d, 8e, 12, 28a-d, 28h and 28i) with IC50s less than 10nM against c-Met. Compou...

journal_title：Bioorganic & medicinal chemistry

authors： Jiang X,Liu H,Song Z,Peng X,Ji Y,Yao Q,Geng M,Ai J,Zhang A

更新日期：2015-02-01 00:00:00

abstract：:3,5-Dihydroxyphenyl decanoate (DPD) is found to inhibit the diphenolase activity of tyrosinase from mushroom (Agaricus bisporus). The effects of DPD on the diphenolase activity of mushroom tyrosinase have been studied. The results show that the enzyme activity decreases very slowly with an increase in DPD concentratio...

journal_title：Bioorganic & medicinal chemistry

authors： Qiu L,Chen QX,Wang Q,Huang H,Song KK

更新日期：2005-11-15 00:00:00

abstract：:Novel pyrazolyl-2,4-thiazolidinediones were prepared via the reaction of appropriate pyrazolecarboxaldehydes with 2,4-thiazolidinediones and substituted benzyl-2,4-thiazolidinediones. The resultant compounds were first evaluated for their anti-inflammatory and neuroprotective properties in vitro. The active compounds ...

journal_title：Bioorganic & medicinal chemistry

authors： Youssef AM,White MS,Villanueva EB,El-Ashmawy IM,Klegeris A

更新日期：2010-03-01 00:00:00

abstract：:Glycamino acids, a family of sugar amino acids, are derivatives of C-glycosides that possesses a carboxyl group at the C-1 position and an amino group replacing one of the hydroxyl groups at either the C-2, 3, 4, or 6 position. We have prepared a series of glucose-type glycamino acids as monomeric building blocks: the...

journal_title：Bioorganic & medicinal chemistry

authors： Suhara Y,Yamaguchi Y,Collins B,Schnaar RL,Yanagishita M,Hildreth JE,Shimada I,Ichikawa Y

更新日期：2002-06-01 00:00:00

abstract：:Betulinic acid (BA), a pentacyclic triterpenoid, exhibits broad spectrum antiproliferative activity, but generally with only modest potency. To improve BA's pharmacological properties, fluorine was introduced as a single atom at C-2, creating two diastereomers, or in a trifluoromethyl group at C-3. We evaluated the im...

journal_title：Bioorganic & medicinal chemistry

authors： Li J,Chang LC,Hsieh KY,Hsu PL,Capuzzi SJ,Zhang YC,Li KP,Morris-Natschke SL,Goto M,Lee KH

更新日期：2019-07-01 00:00:00

abstract：:The problem of predicting torsadogenic cardiotoxicity of drugs is afforded in this work. QSAR studies on a series of molecules, acting as hERG K+ channel blockers, were carried out for this purpose by using the CODESSA program. Molecules belonging to the analyzed dataset are characterized by different therapeutic targ...

journal_title：Bioorganic & medicinal chemistry

authors： Coi A,Massarelli I,Murgia L,Saraceno M,Calderone V,Bianucci AM

更新日期：2006-05-01 00:00:00

abstract：:The β-lactam antibiotic resistance of Gram-negative bacteria has shown to be a critical global health problem. One of the primary reasons for the drug resistance is the existence of β-lactamases especially metallo-β-lactamases such as New Delhi metallo-β-lactamase (NDM-1) and Verona Integron-encoded metallo-β-lactamas...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang J,Wang S,Wei Q,Guo Q,Bai Y,Yang S,Song F,Zhang L,Lei X

更新日期：2017-10-01 00:00:00

abstract：:A quantitative structure-activity relationship (QSAR) study has been made on two different series of tetrahydropyrimidinones acting as HIV-1 protease inhibitors. A structural parameter, the first order valence molecular connectivity index ((1)chi(v)), has been used to account for the variation in the activity. The pro...

journal_title：Bioorganic & medicinal chemistry

authors： Gayathri P,Pande V,Sivakumar R,Gupta SP

更新日期：2001-11-01 00:00:00

abstract：:Four novel scaffolds consisting of total 24 compounds (1a-1o, 2a-2c, 3a-3c and 4a-4c) bearing aromatic sulfonamide and coumarin moieties connected through various linkers were synthesized in order to synergize the inhibition potential of both the moieties against four selected human carbonic anhydrase isoforms (hCA I,...

journal_title：Bioorganic & medicinal chemistry

authors： Chandak N,Ceruso M,Supuran CT,Sharma PK

更新日期：2016-07-01 00:00:00

abstract：:Human dipeptidyl peptidase I (hDPPI, cathepsin C, EC 3.4.14.1) is a novel putative drug target for the treatment of inflammatory diseases. Using 1 as a starting point (IC50>10 microM), we have improved potency by more than 500-fold and successfully identified novel inhibitors of DPPI via screening of a one-bead-two-co...

journal_title：Bioorganic & medicinal chemistry

authors： Bondebjerg J,Fuglsang H,Valeur KR,Kaznelson DW,Hansen JA,Pedersen RO,Krogh BO,Jensen BS,Lauritzen C,Petersen G,Pedersen J,Naerum L

更新日期：2005-07-15 00:00:00

abstract：:Phenylacetate induced tumor cytostasis and differentiation. The chemotherapeutic function of the compound in lung cancer has been previously reported, however, whether or not phenylacetate performs other activities is not known. In this study, the potential usage of synthetic phenylacetate derivatives, 4-fluoro-N-buty...

journal_title：Bioorganic & medicinal chemistry

authors： Liu CH,Huang LJ,Kuo SC,Lee TH,Tsai KJ,Chan HC

更新日期：2009-01-01 00:00:00

abstract：:Three series of new N-substituted 1,2,3,4-tetrahydroisoquinolines with 2-, 3-, and 4-membered alkyl chains (a, b, and c, respectively) were synthesized, and the effect of some structural modifications on their 5-HT1A receptor affinities and functional properties was discussed. It was found that the volume of the termi...

journal_title：Bioorganic & medicinal chemistry

authors： Mokrosz MJ,Bojarski AJ,Duszyńska B,Tatarczyńska E,Kłodzińska A,Dereń-Wesołek A,Charakchieva-Minol S,Chojnacka-Wójcik E

更新日期：1999-02-01 00:00:00

abstract：:A library of novel 2,5-disubtituted-1,3,4-oxadiazoles with benzimidazole backbone (3a-3r) was synthesized and evaluated for their potential as β-glucuronidase inhibitors. Several compounds such as 3a-3d, 3e-3j, 3l-3o, 3q and 3r showed excellent inhibitory potentials much better than the standard (IC50=48.4±1.25μM: d-s...

journal_title：Bioorganic & medicinal chemistry

authors： Zawawi NK,Taha M,Ahmat N,Wadood A,Ismail NH,Rahim F,Ali M,Abdullah N,Khan KM

更新日期：2015-07-01 00:00:00

abstract：:A novel series of indole and benzimidazole derivatives were synthesized and evaluated for their inhibitory activity of rat prostatic 5alpha-reductase. Among these compounds, 4-¿2-[1-(4,4'-dipropylbenzhydryl)indole-5-carboxamido]phenoxy¿buty ric acid (15) and its benzimidazole analogue 25 showed potent inhibitory activ...

journal_title：Bioorganic & medicinal chemistry

authors： Takami H,Kishibayashi N,Ishii A,Kumazawa T

更新日期：1998-12-01 00:00:00

abstract：:The recent price explosion of important agricultural commodities has lead to an international food crisis. The price rise is attributed to fundamental factors, such as the rising demand for dairy and meat products in China and the development of the bioenergy branch as well as on short-term factors such as the behavio...

journal_title：Bioorganic & medicinal chemistry

authors： Schmitz PM,Kavallari A

更新日期：2009-06-15 00:00:00

abstract：:A series of novel flurbiprofen-clioquinol hybrids were designed and synthesized as multifunctional agents for Alzheimer's disease therapy, and their potential was evaluated through various biological experiments. In vitro studies showed that most target compounds exhibited significant ability to inhibit self- and Cu2+...

journal_title：Bioorganic & medicinal chemistry

authors： Yang Z,Song Q,Cao Z,Yu G,Liu Z,Tan Z,Deng Y

更新日期：2020-04-01 00:00:00

abstract：:The activated vitamin D3 derivative 26,27-F6-1alpha,25(OH)2D3 (2a), its three A-ring diastereomers (2b, 2c, 2d), and 5,6-trans isomer (2e) were prepared. Two analogues (2b, 2c) of these isomers were synthesized by a palladium catalyzed coupling reaction using vinyl bromide 5 and enynes (6a, 6b), which were derived fro...

journal_title：Bioorganic & medicinal chemistry

authors： Ikeda M,Takahashi K,Dan A,Koyama K,Kubota K,Tanaka T,Hayashi M

更新日期：2000-08-01 00:00:00

abstract：:The piperazine ring of the potent nootropic drug DM235 has been decorated with H-bond donor and acceptor groups (CH2OH, CH2OMe, CH2OCOMe, COOEt); the aim was to insert new functional groups, suitable for further chemical manipulation. The influence of these modifications on nootropic activity was assessed by means of ...

journal_title：Bioorganic & medicinal chemistry

authors： Martino MV,Guandalini L,Di Cesare Mannelli L,Menicatti M,Bartolucci G,Dei S,Manetti D,Teodori E,Ghelardini C,Romanelli MN

更新日期：2017-03-15 00:00:00

abstract：:Structure-activity relationships of amide-phosphonate derivatives as inhibitors of the human soluble epoxide hydrolase (sEH) were investigated. First, a series of alkyl or aryl groups were substituted on the carbon alpha to the phosphonate function in amide compounds to see whether substituted phosphonates can act as ...

journal_title：Bioorganic & medicinal chemistry

authors： Kim IH,Park YK,Nishiwaki H,Hammock BD,Nishi K

更新日期：2015-11-15 00:00:00

abstract：:This report describes the synthesis and evaluation of glycosylated polyacrylate nanoparticles that have covalently-bound antibiotics within their framework. The requisite glycosylated drug monomers were prepared from one of three known antibiotics, an N-sec-butylthio beta-lactam, ciprofloxacin, and a penicillin, by ac...

journal_title：Bioorganic & medicinal chemistry

authors： Abeylath SC,Turos E,Dickey S,Lim DV

更新日期：2008-03-01 00:00:00