Anti-HIV activity of stilbene-related heterocyclic compounds.

abstract：:This work demonstrated the high efficiency of a sub-milligram-synthesis based medicinal chemistry method. Totally 72 compounds, consisting a tri-substituted pyrrolidine core, were prepared. Around 0.1mg of each compound was solid-phase synthesized. Based on the additive property of UV absorptions of unconjugated chrom...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tian Y,Jin J,Wang C,Lv W,Li X,Che X,Gong Y,Li Y,Li Q,Hou J,Wang PG,Shen J

更新日期：2016-05-15 00:00:00

abstract：:We report the results of our study into a series of simple phenyl and alkyl sulfamates and alkyl methanesulfonates as potential inhibitors of the enzyme estrone sulfatase (ES). The results of the study show that the substituted phenyl sulfamates are good irreversible inhibitors; the alkyl sulfamate compounds were foun...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ahmed S,James K,Owen CP,Patel CK,Sampson L

更新日期：2002-05-06 00:00:00

abstract：:A novel fluorescein-based fluorescent probe for nitroxyl (HNO) based on the reductive Staudinger ligation of HNO with an aromatic phosphine was prepared. This probe reacts with HNO derived from Angeli's salt and 4-bromo Piloty's acid under physiological conditions without interference by other biological redox species...

journal_title：Bioorganic & medicinal chemistry letters

authors： Miao Z,Reisz JA,Mitroka SM,Pan J,Xian M,King SB

更新日期：2015-01-01 00:00:00

abstract：:A series of 1-isoquinolinylguanidines are shown to be potent inhibitors of uPA with selectivity over tPA and plasmin. Potency is enhanced by the presence of a 4-halo and a 7-aryl substituent, particularly when substituted by a 3-carboxylic acid group. Compound 13j (UK-356,202) combines excellent potency and selectivit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Barber CG,Dickinson RP,Fish PV

更新日期：2004-06-21 00:00:00

abstract：:A small set of 9-aminoacridine-3- and 4-carboxamides were synthesized efficiently using the benzyne/azide click chemistry. The products bind to duplex DNA but have different antitumour activity in the HL60 cell line. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Howell LA,Howman A,O'Connell MA,Mueller A,Searcey M

更新日期：2009-10-15 00:00:00

abstract：:Aiming to develop a new (99m)Tc-labeled folate derivative for FR-positive tumor imaging, a simpler method has been established to synthesize the folate-drug conjugates with free α-carboxyl group. In this study, the conjugate pteroyl-lys-HYNIC was synthesized and labeled with (99m)Tc using tricine and TPPTS as co-ligan...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guo H,Xie F,Zhu M,Li Y,Yang Z,Wang X,Lu J

更新日期：2011-04-01 00:00:00

abstract：:New analogues of the venerable antimalarial drug primaquine have been synthesized and bioassayed in vivo against Pneumocystis carinii, a life-threatening infection common among immunosuppressed patients. Two of these new compounds are significantly more active than primaquine itself, and provide new information for fu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Goodwin TE,Boylan CJ,Current WL,Byrd JC,Edwards CB,Fuller DA,Green JL,Larocca CD,Raney KD,Ross AS,Tucker WA

更新日期：2000-10-02 00:00:00

abstract：:Design, synthesis, and SAR of 7-oxopyrrolopyridine-derived DPP4 inhibitors are described. The preferred stereochemistry of these atropisomeric biaryl analogs has been identified as Sa. Compound (+)-3t, with a K(i) against DPP4, DPP8, and DPP9 of 0.37 nM, 2.2, and 5.7 μM, respectively, showed a significant improvement ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang W,Devasthale P,Wang A,Harrity T,Egan D,Morgan N,Cap M,Fura A,Klei HE,Kish K,Weigelt C,Sun L,Levesque P,Li YX,Zahler R,Kirby MS,Hamann LG

更新日期：2011-11-15 00:00:00

abstract：:Several unnatural derivatives of narciclasine were prepared in which the C-7 carbon was replaced with nitrogen. The 7-aza derivative and its N-oxide were prepared by the coupling of iodopicolinic acid with a conduramine unit derived chemoenzymatically from bromobenzene. Intramolecular Heck reaction was used to constru...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vshyvenko S,Reisenauer MR,Rogelj S,Hudlicky T

更新日期：2014-09-01 00:00:00

abstract：:The thrombin receptor (PAR-1) is activated by alpha-thrombin to stimulate various cell types, including platelets, through the tethered-ligand sequence SFLLRN. Macrocyclic peptide analogues of SFLLRN were synthesized and evaluated in vitro. In general, the compounds were much less potent in inducing platelet aggregati...

journal_title：Bioorganic & medicinal chemistry letters

authors： McComsey DF,Hecker LR,Andrade-Gordon P,Addo MF,Maryanoff BE

更新日期：1999-01-18 00:00:00

abstract：:A new series of triazole-imidazo[2,1-b][1,3,4]thiadiazole hybrids (6a-s, 7a) were designed by a molecular hybridisation approach and the target molecules were synthesized via one pot click chemistry protocol. All the intermediates and final molecules were characterised using spectral methods and one of the target comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ramprasad J,Nayak N,Dalimba U,Yogeeswari P,Sriram D

更新日期：2015-10-01 00:00:00

abstract：:Relying on the high affinities of the benz-indolo-azecine LE 300 (1) and the hydroxylated dibenz-azecine LE 404 (2b) for the D1/D5 receptor subtypes, we synthesized methoxylated, hydroxylated and an indole-N methylated derivatives of 1 (Fig. 1). Hydroxylation of azecine derivatives is beneficial with regard to the aff...

journal_title：Bioorganic & medicinal chemistry letters

authors： Enzensperger C,Kilian S,Ackermann M,Koch A,Kelch K,Lehmann J

更新日期：2007-03-01 00:00:00

abstract：:The chemical resolution, using N-tosyl-L-proline as a chiral auxiliary, of a racemate of the pyrazole analog (+/-)-N-Boc-CPzI of the left hand segment (CPI) of the antitumor agent CC-1065, and the cytotoxic evaluation of both enantiomers are described. The reported results further validate the direct relationship betw...

journal_title：Bioorganic & medicinal chemistry letters

authors： Baraldi PG,Cacciari B,Romagnoli R,Spalluto G,Boyce CW,Boger DL

更新日期：1999-11-01 00:00:00

abstract：:A series of 5-substitutedbenzylideneamino-2-butylbenzofuran-3-yl-4-methoxyphenyl methanones is synthesized and evaluated for antileishmanial and antioxidant activities. Compounds 4f (IC50 = 52.0 ± 0.09 µg/ml), 4h (IC50 = 56.0 ± 0.71 µg/ml) and 4l (IC50 = 59.3 ± 0.55 µg/ml) were shown significant antileishmanial when c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patil SR,Bollikonda S,Patil RH,Sangshetti JN,Bobade AS,Asrondkar A,Reddy PP,Shinde DB

更新日期：2018-02-01 00:00:00

abstract：:The synthesis of 22 2-aryl-1H-indoles, including 12 new compounds, has been achieved via Pd- or Rh-mediated methodologies, or selective electrophilic substitution. All three methods were based on elaborations from simple indole precursors. SAR studies on these indoles and 2-phenyl-1H-indole in Staphylococcus aureus as...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ambrus JI,Kelso MJ,Bremner JB,Ball AR,Casadei G,Lewis K

更新日期：2008-08-01 00:00:00

abstract：:Exogenous short-chain nucleic acids undergo rapid import into the nucleus. Fluorescence-labeled dT1-13 DNA microinjected into the cytoplasm domain of a HeLa cell was rapidly imported into the nucleus domain within 1min. This is much more rapid than what has been observed for intracellular diffusion of small molecules....

journal_title：Bioorganic & medicinal chemistry letters

authors： Kitagawa M,Okamoto A

更新日期：2016-10-01 00:00:00

abstract：:Perfluorination of phthalimides leads to dramatically increased potency as inhibitors of TNF-alpha production. We examined the enantiodependence for several tetrafluorophthalimides and alpha-methylthalidomide, 3. Only 3 exhibited strikingly enantiodependent activity. The key structural determinant for the enhanced act...

journal_title：Bioorganic & medicinal chemistry letters

authors： Niwayama S,Loh C,Turk BE,Liu JO,Miyachi H,Hashimoto Y

更新日期：1998-05-05 00:00:00

abstract：:A novel series of potent histamine H(3) receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold has been discovered. Several compounds display high selectivity over other histamine receptor subtypes and have favorable physicochemical properties, low potential for CYP450 enzyme inhibit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Richter HG,Freichel C,Huwyler J,Nakagawa T,Nettekoven M,Plancher JM,Raab S,Roche O,Schuler F,Taylor S,Ullmer C,Wiegand R

更新日期：2010-10-01 00:00:00

abstract：:A novel, potent, and orally bioavailable class of product-like inhibitors of the HCV NS3 protease was discovered by constraining the P2-P3 amide bond and the P3 hydrocarbon substituent to the protease-bound conformation. This preorganization was accomplished by incorporation of the P2-P3 amide into a six-membered ring...

journal_title：Bioorganic & medicinal chemistry letters

authors： Clarke MO,Byun D,Chen X,Doerffler E,Leavitt SA,Sheng XC,Yang CY,Kim CU

更新日期：2012-01-15 00:00:00

abstract：:The present work reports on the preparation of glass surfaces coated with NPPOC-protected aminooxy groups and their use for the patterning of oligonucleotides on glass slides and in capillary tubes. The method involves the use of surfaces coated with amino groups using (gamma-aminopropyl)triethoxy silane and subsequen...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dendane N,Hoang A,Defrancq E,Vinet F,Dumy P

更新日期：2008-04-15 00:00:00

abstract：:A facile synthesis of 7-epi-(-)-goniofufurone as well as the first synthesis of (-)-crassalactone C was achieved starting from D-xylose. A comparison of their in vitro antitumour activities with those observed for the corresponding naturally occurring enantiomers was provided. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Popsavin V,Benedeković G,Srećo B,Popsavin M,Francuz J,Kojić V,Bogdanović G

更新日期：2008-10-01 00:00:00

abstract：:Multidrug resistance in tumor cells poses a major obstacle to efficient chemotherapy. Several types of agents have been recognized as multidrug resistance inhibitors, among which the tetrahydroisoquinolines is the most studied. In current study 16 furoxan-based nitric oxide-releasing derivatives of tetrahydroisoquinol...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zou ZH,Lan XB,Qian H,Huang WL,Li YM

更新日期：2011-10-01 00:00:00

abstract：:(+)-proto-Quercitol (1) and (-)-vibo-quercitol (2), both of which could be readily prepared by the bioconversion of myo-inositol, were successfully converted into the corresponding 4-methylenecyclohex-5-ene-1,2,3-triol derivatives. These compounds were demonstrated to be suitable precursors, preserving their configura...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kuno S,Takahashi A,Ogawa S

更新日期：2011-12-01 00:00:00

abstract：:A series of naphthalenyloxy-arylpropylamines have been prepared and are demonstrated to be inhibitors of both serotonin and norepinephrine reuptake. One member of this series, duloxetine (Cymbalta) has proven to be effective in clinical trials for the treatment of depression. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bymaster FP,Beedle EE,Findlay J,Gallagher PT,Krushinski JH,Mitchell S,Robertson DW,Thompson DC,Wallace L,Wong DT

更新日期：2003-12-15 00:00:00

abstract：:The rational design, syntheses and evaluation of potent sulfonamidopyrrolidin-2-one-based factor Xa inhibitors incorporating aminoindane and phenylpyrrolidine P4 motifs are described. These series delivered highly potent anticoagulant compounds with excellent oral pharmacokinetic profiles; however, significant time de...

journal_title：Bioorganic & medicinal chemistry letters

authors： Young RJ,Adams C,Blows M,Brown D,Burns-Kurtis CL,Chan C,Chaudry L,Convery MA,Davies DE,Exall AM,Foster G,Harling JD,Hortense E,Irvine S,Irving WR,Jackson S,Kleanthous S,Pateman AJ,Patikis AN,Roethka TJ,Senger S,

更新日期：2011-03-15 00:00:00

abstract：:Mycoepoxydiene (MED) is a polyketide isolated from a marine fungus associated with mangrove forests. It contains an oxygen-bridged cyclooctadiene core and an α,β-unsaturated δ-lactone moiety. MED induced the reorganization of cytoskeleton in actively growing HeLa cells by promoting formation of actin stress fiber and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang J,Zhao B,Zhang W,Wu X,Wang R,Huang Y,Chen D,Park K,Weimer BC,Shen Y

更新日期：2010-12-01 00:00:00

abstract：:New polyphenol classes have been tested against amyloid-beta peptide aggregation. We have identified four novel polyphenols which could be efficient fibril inhibitors in Alzheimer's disease: malvidin and its glucoside and curculigosides B and D. We suggest that molecules with the particular C(6)-linkers-C(6) structure...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rivière C,Richard T,Vitrac X,Mérillon JM,Valls J,Monti JP

更新日期：2008-01-15 00:00:00

abstract：:AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100nM inhibitor of Lp-PLA(2). However, in the presence of EDTA the inhibitory activity of AX10185 was extinguished while the enzymatic activity of Lp-PLA(2) did not change. Subsequent metal screening experiments determined the inhibition to be Zn(2+)...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lin EC,Hu Y,Amantea CM,Pham LM,Cajica J,Okerberg E,Brown HE,Fraser A,Du L,Kohno Y,Ishiyama J,Kozarich JW,Shreder KR

更新日期：2012-01-15 00:00:00

abstract：:Different types of heterogenized catalysts were involved in asymmetric reactions. Hydrogen transfer reduction was performed with amino alcohols derived from poly((S)-(GMA-co-EGDMA or DVB)) and hydrogenation with BINAP grafted onto PEG or copolymerized with isocyanates as ligands. Attempts of catalysts recycling are re...

journal_title：Bioorganic & medicinal chemistry letters

authors： Saluzzo C,Lamouille T,Hérault D,Lemaire M

更新日期：2002-07-22 00:00:00

abstract：:Distamycin and nitrogen mustard conjugates, in which the nitrogen mustard unit was coupled to the C-terminus of the pyrrole, were synthesized. The switching of the nitrogen mustard unit from the N-terminus to the C-terminus did not compromise the compound's cytotoxicity. Compound 3, bearing three pyrrole units, was hi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang Y,Wright SC,Larrick JW

更新日期：2003-02-10 00:00:00