Selective inactivation of triosephosphate isomerase from Trypanosoma cruzi by brevifolin carboxylate derivatives isolated from Geranium bellum Rose.

abstract：:The growth inhibition of human cancer cells via T-type Ca(2+) channel blockade has been well known. Herein, a series of new 3,4-dihydroquinazoline derivatives were synthesized via a brief SAR study on KYS05090 template and evaluated for both T-type Ca(2+) channel (Cav3.1) blockade and cytotoxicity on three human ovari...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jang SJ,Choi HW,Choi DL,Cho S,Rim HK,Choi HE,Kim KS,Huang M,Rhim H,Lee KT,Lee JY

更新日期：2013-12-15 00:00:00

abstract：:A new family of photonuclease, thiadiazole-naphthalimide were synthesized and evaluated. Thiadiazole group was incorporated for the first time. These compounds intercalated into DNA efficiently and damaged DNA as low as 10 microM photochemically. Mechanism experiment showed that electron transfer and radicals were inv...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li Y,Xu Y,Qian X,Qu B

更新日期：2003-10-20 00:00:00

abstract：:The first demonstration of DNA cleavage by resveratrol '3,5,4'-trihydroxy-trans-stilbene' is presented. Resveratrol mediated relaxation of pBR322 at micromolar concentrations in the presence of Cu2+. Evidence is provided that resveratrol is capable of binding to DNA, and that the Cu(2+)-dependent DNA damage is more li...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fukuhara K,Miyata N

更新日期：1998-11-17 00:00:00

abstract：:A series of human carbonic anhydrase (hCA) IX inhibitors conjugated to various near-infrared fluorescent dyes was synthesized with the aim of imaging hypoxia-induced hCA IX expression in tumor cells in vitro, ex vivo and in vivo. The resulting compounds were profiled for inhibition of transmembrane hCA IX showing a ra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Groves K,Bao B,Zhang J,Handy E,Kennedy P,Cuneo G,Supuran CT,Yared W,Peterson JD,Rajopadhye M

更新日期：2012-01-01 00:00:00

abstract：:The convergent synthesis of C35-fluorinated analogues of solamin, a mono-THF Annonaceous acetogenin, has been achieved by the Sonogashira coupling of the THF ring fragment and the fluorinated γ-lactone fragment. It was revealed that the number of fluorine atoms on the γ-lactone moiety affects the growth inhibitory act...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kojima N,Suga Y,Hayashi H,Yamori T,Yoshimitsu T,Tanaka T

更新日期：2011-10-01 00:00:00

abstract：:Eighteen diamidino azaterphenyls and analogues were evaluated as anti-leishmanials; nine of the compounds gave IC50 values less than 1 microM, five exhibited values less than 0.40 microM, and two gave values less than 0.10 microM in a Leishmania donovani axenic amastigote assay. The activity of the diamidines strongly...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hu L,Arafa RK,Ismail MA,Wenzler T,Brun R,Munde M,Wilson WD,Nzimiro S,Samyesudhas S,Werbovetz KA,Boykin DW

更新日期：2008-01-01 00:00:00

abstract：:A series of benzoxazole/benzothiazole-2,3-dihydrobenzo[b][1,4]dioxine derivatives (5a-5d and 8a-8j) was synthesized. Compounds were evaluated for binding affinities at the 5-HT1A and 5-HT2A receptors. Antidepressant activities of the compounds were screened using the forced swimming test (FST) and the tail suspension ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang S,Chen Y,Zhao S,Xu X,Liu X,Liu BF,Zhang G

更新日期：2014-04-01 00:00:00

abstract：:A series of pyrrolo[3,2,1-ij]quinoline derivatives was synthesized, evaluated for their activity against the 5-HT2c and 5-HT2a, receptors and found to be agonists at 5-HT2c with selectivity over 5-HT2a. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Isaac M,Slassi A,O'Brien A,Edwards L,MacLean N,Bueschkens D,Lee DK,McCallum K,De Lannoy I,Demchyshyn L,Kamboj R

更新日期：2000-05-01 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 series of orthoalkylaminophenol derivatives was synthesized and tested in vitro with respect to their neuroprotective effect. Some of these compounds exhibited a potent antioxidant activity close to that of standard alpha-tocopherol. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Larget R,Lockhart B,Pfeiffer B,Neudorffer A,Fleury MB,Largeron M

更新日期：1999-10-18 00:00:00

abstract：:Quinolizidinyl derivatives of the tricyclic systems characterizing pirenzepine and nuvenzepine, were prepared and tested as ligands for muscarinic M1, M2 and M3 receptors; 5,11-dihydro-11-[(S-lupinyl)-thioacetyl]-6H-pyrido[2,3-b][1, 4]benzodiazepin-6-one exhibited IC50 = 10 nM for M1 and 760 nM for both M2 and M3 subt...

journal_title：Bioorganic & medicinal chemistry letters

authors： Novelli F,Sparatore A,Tasso B,Sparatore F

更新日期：1999-10-18 00:00:00

abstract：:The synthesis and biological evaluation of novel human A-FABP inhibitors based on the 6-(trifluoromethyl)pyrimidine-4(1H)-one scaffold is described. Two series of compounds, bearing either an amino or carbon substituent in the 2-position of the pyrimidine ring were investigated. Modification of substituents and chain ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ringom R,Axen E,Uppenberg J,Lundbäck T,Rondahl L,Barf T

更新日期：2004-09-06 00:00:00

abstract：:New adjuvants of warfarin anticoagulant activity have been developed. These compounds, which are 1,4-methano-1,2,3,4-tetrahydroanthracene-9,10-diol derivatives, act synergistically with warfarin to potentiate its anticoagulant effect. None of the compounds tested is an effective oral anticoagulant in the absence of wa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Stromich JJ,Weber AK,Mirzaei YR,Caldwell MD,Lewis DE

更新日期：2010-03-15 00:00:00

abstract：:To investigate the stability of 2'-C-cyano-2'-deoxy-1-beta-D-arabino-pentafuranosylcytosine 3'-phosphoric acid, its thymidine ester was prepared via the phosphoramidite method using allyl protection for the phosphate function. This ester is stable under acidic conditions but extremely labile under basic conditions, de...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hayakawa Y,Kawai R,Otsuki K,Kataoka M,Matsuda A

更新日期：1998-09-22 00:00:00

abstract：:The underlying mechanisms of urocanic acid (UA) to induce immune suppression remain elusive until the recent finding that cis-UA acts via the serotonin, 5-hydroxytryptamine (5-HT) receptor subtype 5-HT(2A). In the present study, the interactions of cis-UA to 5-HT(2A) receptor were explored and compared with those of 5...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shen L,Ji HF

更新日期：2009-09-15 00:00:00

abstract：:Catalytic disulfenylation reaction of alkenes by common Lewis acids has been investigated in detail. While reactions by FeCl(3) were feasible with cycloalkenes and other simple alkenes, much faster and excellent conversions were possible by AlCl(3) even with the substrates less reactive toward FeCl(3). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yamagiwa N,Suto Y,Torisawa Y

更新日期：2007-11-15 00:00:00

abstract：:A series of 2-phenylspiroindenediones was prepared. The spiroindenediones were found to be less active than the corresponding spiroindenes as estrogen receptor ligands and failed to demonstrate the receptor subtype selectivity that had been anticipated from molecular modeling. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Blizzard TA,Mosley RT,Birzin ET,Chan W,Hammond ML

更新日期：2004-03-08 00:00:00

abstract：:(3-tert-Butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)pyrazolo[1,5-d][1,2,4]triazine (1) was recently identified as a functionally selective, inverse agonist at the benzodiazepine site of GABA(A) alpha5 receptors and enhances performance in animal models of cognition. The routes of metabolis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jones P,Atack JR,Braun MP,Cato BP,Chambers MS,O'Connor D,Cook SM,Hobbs SC,Maxey R,Szekeres HJ,Szeto N,Wafford KA,MacLeod AM

更新日期：2006-02-15 00:00:00

abstract：:The discovery of potent benzimidazole stearoyl-CoA desaturase (SCD1) inhibitors by ligand-based virtual screening is described. ROCS 3D-searching gave a favorable chemical motif that was subsequently optimized to arrive at a chemical series of potent and promising SCD1 inhibitors. In particular, compound SAR224 was se...

journal_title：Bioorganic & medicinal chemistry letters

authors： Matter H,Zoller G,Herling AW,Sanchez-Arias JA,Philippo C,Namane C,Kohlmann M,Pfenninger A,Voss MD

更新日期：2013-03-15 00:00:00

abstract：:A series of tertiary amine analogs derived from lead azaaromatic quaternary ammonium salts has been designed and synthesized. The preliminary structure-activity relationships of these new analogs suggest that such tertiary amine analogs, which potently inhibit nicotine-evoked dopamine release from rat striatum, repres...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang Z,Zheng G,Pivavarchyk M,Deaciuc AG,Dwoskin LP,Crooks PA

更新日期：2011-01-01 00:00:00

abstract：:The synthesis and antihypertensive activity of racemates and enantiomers of substituted 2,3,8,8a-tetrahydro-7H-oxazolo[3,2-a]pyridinedicarboxylates have been reported. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Martín E,Morán A,Martín ML,San Román L,Puebla P,Medarde M,Caballero E,San Feliciano A

更新日期：2000-02-21 00:00:00

abstract：:From an easily available partially protected formal derivative of 1-deoxymannojirimycin, by hydroxymethyl chain-branching and further elaboration, lipophilic analogs of the powerful β-d-galactosidase inhibitor 4-epi-isofagomine have become available. New compounds exhibit improved inhibitory activities comparable to b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thonhofer M,Weber P,Santana AG,Fischer R,Pabst BM,Paschke E,Schalli M,Stütz AE,Tschernutter M,Windischhofer W,Withers SG

更新日期：2016-03-01 00:00:00

abstract：:The bacterium responsible for tuberculosis is increasing its resistance to antibiotics resulting in new multidrug-resistant Mycobacterium tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB). In this study, several analytical techniques including NMR, FT-ICR, MALDI-MS, LC-MS and UV/Vis are used t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Manning T,Mikula R,Wylie G,Phillips D,Jarvis J,Zhang F

更新日期：2015-02-01 00:00:00

abstract：:Six N-nitroaryl-2-amino-1,3-dichloropropane derivatives have been prepared and evaluated against 18 cancer cell lines and two non-cancerous cell lines. Analysis of cell viability data and IC50 values indicated that the presence of a trifluoromethyl group in the nitroaryl moiety is an important structural feature assoc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chappel L,Wong LC,Leong CO,Mai CW,Meikle IT,Stanforth SP,Truong TV

更新日期：2020-02-15 00:00:00

abstract：:Fifteen new alpha-acylaminoketones were prepared by four different routes in an initial effort to optimize the potency of these compounds as ecdysone agonists. The compounds were assayed in mammalian cells expressing the ecdysone receptors from Bombyx mori (BmEcR) and Choristoneura fumiferana (CfEcR) for their ability...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tice CM,Hormann RE,Thompson CS,Friz JL,Cavanaugh CK,Saggers JA

更新日期：2003-06-02 00:00:00

abstract：:A novel conjugate of Hoechst 33258, pyrene and neomycin was synthesized and examined for its binding and stabilization of A-T rich DNA duplexes using spectroscopic and viscometric techniques. The conjugate, containing three well known ligands that bind nucleic acids albeit in different binding modes, was found to sign...

journal_title：Bioorganic & medicinal chemistry letters

authors： Willis B,Arya DP

更新日期：2009-09-01 00:00:00

abstract：:A series of anthranilodinitrile-based biaryls were synthesized and evaluated in vitro against extracellular promastigotes and intracellular amastigotes of Leishmania donovani. Among various screened compounds, a biaryl with trifluoromethyl group 5f showed 83% inhibition against promastigotes and 70% inhibition against...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh FV,Vatsyayan R,Roy U,Goel A

更新日期：2006-05-15 00:00:00

abstract：:The synthesis and evaluation of tetrasubstituted aminopyridines, bearing novel azaindazole hinge binders, as potent AKT inhibitors are described. Compound 14c was identified as a potent AKT inhibitor that demonstrated reduced CYP450 inhibition and an improved developability profile compared to those of previously desc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lin H,Yamashita DS,Xie R,Zeng J,Wang W,Leber J,Safonov IG,Verma S,Li M,Lafrance L,Venslavsky J,Takata D,Luengo JI,Kahana JA,Zhang S,Robell KA,Levy D,Kumar R,Choudhry AE,Schaber M,Lai Z,Brown BS,Donovan BT,Mi

更新日期：2010-01-15 00:00:00

abstract：:A novel diamino-substituted hypocrellin derived from hypocrellin B (HB) was synthesized by a mild method. The red absorption of the resulting product was significantly enhanced relative to the parent hypocrellins and any other hypocrellin derivatives, and the active oxygen species generating abilities were enhanced di...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu S,Chen S,Zhang M,Shen T

更新日期：2004-03-22 00:00:00

abstract：:Chalcone type compound 1a ((E)-6'-benzylidene-4a'-methyl-4',4a',7',8'-tetrahydro-3'H-spiro[[1,3]dithiolane-2,2'-naphthalen]-5'(6'H)-one) was discovered as an potent inhibitor in melanogenesis. To define its structure-activity relationship, a series of analogs 1b-n, dithiolane truncated 2a-b and ring A removed 3a-e wer...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thanigaimalai P,Lee KC,Sharma VK,Rao EV,Roh E,Kim Y,Jung SH

更新日期：2011-04-01 00:00:00