Genotoxic activity of halogenated phenylglycine derivatives.

abstract：:The structures of the uracil and thiouracils were examined using NMR spectroscopy and crystal structure data when available. The relationships between the extent of polarization and the C5-C6 bond length as well as the H5-H6 coupling constants were probed. It was found that the bond length and coupling constants corre...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang S,Gronert S,Wu W

更新日期：2011-11-01 00:00:00

abstract：:Novel polyhalo 2,4-diaminoquinazolines 3a-3d were prepared by reacting polyhaloisophthalonitriles with guanidine carbonate under solvent-free conditions and in the absence of a catalyst with good yields (74-95%). A series of highly functionalized 2,4-diaminoquinazolines 4-5 were then synthesized based on 3a-3c. The an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yan SJ,Zheng H,Huang C,Yan YY,Lin J

更新日期：2010-08-01 00:00:00

abstract：:Guided by X-ray crystallography, we have extended the structure-activity relationship (SAR) study on an isoxazole carboxylic acid-based PTP1B inhibitor (1) and more potent and equally selective (>20-fold selectivity over the highly homologous T-cell PTPase, TCPTP) PTP1B inhibitors were identified. Inhibitor 7 demonstr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao H,Liu G,Xin Z,Serby MD,Pei Z,Szczepankiewicz BG,Hajduk PJ,Abad-Zapatero C,Hutchins CW,Lubben TH,Ballaron SJ,Haasch DL,Kaszubska W,Rondinone CM,Trevillyan JM,Jirousek MR

更新日期：2004-11-15 00:00:00

abstract：:A series of novel methyl 5-substituted 1H-benzo[d]imidazol-2-ylcarbamates were designed, synthesized, and their acrosin inhibitory activities evaluated in vitro. The results of acrosin inhibitory activity showed that all title compounds were more potent than the control TLCK. Compound 4w displayed the most potent acro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu X,Chen Q,Zhu J,Fan Y,Ding L,Zhao J,Han G,Tian W,Qi J,Zhou Y,Lv J

更新日期：2012-05-15 00:00:00

abstract：:New N-(1,2-diphenylethyl)piperazines 6 are disclosed as dual serotonin and noradrenaline reuptake inhibitors (SNRI) which may have potential in treating stress urinary incontinence (SUI). In this Letter, we present new data for SNRI PF-526014 (4) including performance in a canine in vivo model of SUI, cardiovascular a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fray MJ,Fish PV,Allan GA,Bish G,Clarke N,Eccles R,Harrison AC,Le Net JL,Phillips SC,Regan N,Sobry C,Stobie A,Wakenhut F,Westbrook D,Westbrook SL,Whitlock GA

更新日期：2010-06-15 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

abstract：:The docking approach for the screening of designed small molecule ligands, led to the identification of a critical arginine residue in peptide deformylase for spiro cyclopropyl PDF inhibitor's extra hydrophobic binding, providing us a useful tool for searching more efficient PDF inhibitors to fight for horrifying anti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lv F,Chen C,Tang Y,Wei J,Zhu T,Hu W

更新日期：2016-08-01 00:00:00

abstract：:A new class of selective nonsteroidal glucocorticoid receptor modulators typified by N-[3-[benzyl-(4-chloro-2-fluoro-benzyl)-amino]-2-methyl-phenyl]-methanesulfonamide 19 has been discovered. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Link JT,Sorensen BK,Patel J,Emery M,Grynfarb M,Goos-Nilsson A

更新日期：2004-05-03 00:00:00

abstract：:Interleukin-2 inducible T-cell kinase (ITK) is a member of the Tec kinase family and is involved with T-cell activation and proliferation. Due to its critical role in acting as a modulator of T-cells, ITK inhibitors could provide a novel route to anti-inflammatory therapy. This work describes the discovery of ITK inhi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cook BN,Bentzien J,White A,Nemoto PA,Wang J,Man CC,Soleymanzadeh F,Khine HH,Kashem MA,Kugler SZ Jr,Wolak JP,Roth GP,De Lombaert S,Pullen SS,Takahashi H

更新日期：2009-02-01 00:00:00

abstract：:Peptides containing Nepsilon-thioacetyl-lysine and Nepsilon-acetyl-lysine were evaluated for their de(thio)acetylation catalyzed by human HDAC8 and SIRT1, two distinct protein deacetylases. Nepsilon-Thioacetyl-lysine was found to be a mimic of Nepsilon-acetyl-lysine for HDAC8-catalyzed reaction, but to confer inhibiti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fatkins DG,Monnot AD,Zheng W

更新日期：2006-07-15 00:00:00

abstract：:Current Letter presents design, synthesis and biological evaluation of a novel series of pyrazolylthiazole carboxylates 1a-1p and corresponding acid derivatives 2a-2p. All 32 novel compounds were tested for their in vivo anti-inflammatory activity by carrageenan-induced rat paw edema method as well as for in vitro ant...

journal_title：Bioorganic & medicinal chemistry letters

authors： Khloya P,Kumar S,Kaushik P,Surain P,Kaushik D,Sharma PK

更新日期：2015-03-15 00:00:00

abstract：:Thirty-two new derivatives of cerpegin (1,1,5-trimethylfuro[3,4-c]pyridine-3,4-dione) were designed and synthesized in high yield by a new method, combining several C(1) and N(5) substituents. All compounds were tested for their inhibitory effect on the CT-L, T-L and PA proteolytic activities of a purified mammalian 2...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hovhannisyan A,Pham TH,Bouvier D,Qin L,Melikyan G,Reboud-Ravaux M,Bouvier-Durand M

更新日期：2013-05-01 00:00:00

abstract：:A unique bicyclic peptide, moroidin (1), from the seeds of Celosia argentea (Amaranthaceae) strongly inhibited the polymerization of tubulin. The stereostructure of moroidin (1) was reinvestigated by spectroscopic data, chemical degradation, and molecular dynamics simulation. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Morita H,Shimbo K,Shigemori H,Kobayashi J

更新日期：2000-03-06 00:00:00

abstract：:A series of seco-A-pentacyclic triterpenoids-3,4-lactone were synthesized and the anti-HBV activities were evaluated in vitro. Several compounds inhibited the secretion of HBV antigen and the replication of HBV DNA in micromolar level. Compounds D7 and D10, seco-A-oleanane-3,4-lactone, suppressed the HBeAg secretion w...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li Z,Min Q,Huang H,Liu R,Zhu Y,Zhu Q

更新日期：2018-05-15 00:00:00

abstract：:4-(Substituted-benzylidine)-2-substituted-5,6-dihydrobenzo[h]quinazoline (5a-p) and 4-(substituted-benzylidine)-2-substituted-3, 4, 5, 6-tetrahydrobenzo[h]quinazoline (6a-p) have been synthesized from 2-(substituted-benzylidine)tetralone-1(3a-d) and several substituted guanidine sulfates(4a-d).These compounds were tes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Agarwal KC,Sharma V,Shakya N,Gupta S

更新日期：2009-09-15 00:00:00

abstract：:The identification of a novel hit compound inhibitor of the protein-protein interaction between the influenza RNA-polymerase PA and PB1 subunits has been accomplished by means of high-throughput screening. A small family of structurally related molecules has been synthesized and biologically evaluated with most of the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kessler U,Castagnolo D,Pagano M,Deodato D,Bernardini M,Pilger B,Ranadheera C,Botta M

更新日期：2013-10-15 00:00:00

abstract：:Two novel series of small-molecule RGD mimetics containing either a substituted pyridone or pyrazinone central constraint were prepared. Modification of the beta-alanine 3-substituent produced compounds that are potent and selective alpha(v)beta(3) antagonists and exhibit a range of physicochemical properties. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Breslin MJ,Duggan ME,Halczenko W,Fernandez-Metzler C,Hunt CA,Leu CT,Merkle KM,Naylor-Olsen AM,Prueksaritanont T,Stump G,Wallace A,Rodan SB,Hutchinson JH

更新日期：2003-05-19 00:00:00

abstract：:SAR studies for the exploration a novel class of anti-human immunodeficiency virus type 1 (HIV-1) agents based on the hematoxylin structure (1) are described. The systematic deoxygenations of 1 including asymmetric synthesis were conducted to obtain a compound showing high potencies for inhibiting the nuclear import a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ishii H,Koyama H,Hagiwara K,Miura T,Xue G,Hashimoto Y,Kitahara G,Aida Y,Suzuki M

更新日期：2012-02-01 00:00:00

abstract：:N-Phthaloyl 3-amino-3-arylpropionic acid analogs of thalidomide that are potent inhibitors of tumor necrosis factor-alpha are reported. These compounds were found to be potent inhibitors of phosphodiesterase 4. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Muller GW,Shire MG,Wong LM,Corral LG,Patterson RT,Chen Y,Stirling DI

更新日期：1998-10-06 00:00:00

abstract：:A series of tacrine-pyrazolo[3,4-b]pyridine hybrids were synthesised and evaluated as dual cholinesterase (ChE) and phosphodiesterase 4D (PDE4D) inhibitors for the treatment of Alzheimer's disease (AD). Compound 10j, which is tacrine linked with pyrazolo[3,4-b]pyridine moiety by a six-carbon spacer, was the most poten...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pan T,Xie S,Zhou Y,Hu J,Luo H,Li X,Huang L

更新日期：2019-08-15 00:00:00

abstract：:To develop more effective antitumor steroidal drugs, we synthesized a library including twenty-two novel cytotoxic 2-alkyloxyl substituted (25R)-spirostan-1,4,6-triene-3-ones and corresponding 1,2,3-triazoles through an abnormal monoepoxide ring-opening/elimination and 'click' reactions. After the cytotoxic evaluation...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lu XF,Yang Z,Huang NY,He HB,Deng WQ,Zou K

更新日期：2015-09-01 00:00:00

abstract：:In this study, a series of carbazole-rhodanine conjugates was synthesized and evaluated for their Topoisomerase II inhibition potency as well as cytotoxicity against a panel of four human cancer cell lines. Among these thirteen compounds, 3a, 3b, 3g, and 3h possessed Topoisomerase II inhibition potency at 20 μM. Mecha...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jiang H,Zhang WJ,Li PH,Wang J,Dong CZ,Zhang K,Chen HX,Du ZY

更新日期：2018-05-01 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 dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur)) have been identified. The synthesis, structure-activity relationships and selectivity against several other ion channels are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vaccaro W,Huynh T,Lloyd J,Atwal K,Finlay HJ,Levesque P,Conder ML,Jenkins-West T,Shi H,Sun L

更新日期：2008-12-15 00:00:00

abstract：:A series of novel 2,4,5-trisubstituted 1,3-thiazole derivatives containing hydrazide-hydrazine, and carboxamide moiety including 46 compounds T were synthesized, and evaluated for their antitumor activity in vitro against a panel of five human cancer cell lines. Eighteen title compounds T displayed higher inhibitory a...

journal_title：Bioorganic & medicinal chemistry letters

authors： He H,Wang X,Shi L,Yin W,Yang Z,He H,Liang Y

更新日期：2016-07-15 00:00:00

abstract：:New ligands for in vivo brain imaging of serotonin transporter (SERT) with single photon emission tomography (SPECT) were prepared and evaluated. An efficient synthesis and radiolabeling of a biphenylthiol, FLIP-IDAM, 4, was accomplished. The affinity of FLIP-IDAM was evaluated by an in vitro inhibitory binding assay ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zheng P,Lieberman BP,Ploessl K,Lemoine L,Miller S,Kung HF

更新日期：2013-02-01 00:00:00

abstract：:This Letter describes the synthesis of two regioisomers of a new class of vesamicol analogs as possible ligands for imaging the vesicular acetylcholine transporter in future PET studies. The two pyrrolovesamicols (±)-6a and (±)-6b were synthesized by nucleophilic ring opening reaction of a tetrahydroindole epoxide pre...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wenzel B,Li Y,Kraus W,Sorger D,Sabri O,Brust P,Steinbach J

更新日期：2012-03-15 00:00:00

abstract：:Oxytocin (OT) is a neuropeptide involved in a wide variety of physiological actions, both peripherally and centrally. Many human studies have revealed the potential of OT to treat autism spectrum disorders and schizophrenia. OT interacts with the OT receptor (OTR) as well as vasopressin 1a and 1b receptors (V1aR, V1bR...

journal_title：Bioorganic & medicinal chemistry letters

authors： Adachi Y,Sakimura K,Shimizu Y,Nakayama M,Terao Y,Yano T,Asami T

更新日期：2017-06-01 00:00:00

abstract：:Peptide-based alpha-ketoamides, alpha-ketoesters and alpha-diketones were designed, synthesized and evaluated against HCV NS3 protease. Alpha-ketoamides have the highest affinity among the three classes, with 8 being the most potent inhibitor with an IC50 of 340 nM. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Han W,Hu Z,Jiang X,Decicco CP

更新日期：2000-04-17 00:00:00

abstract：:Several oximes of triterpenes with a 17-beta hydroxyl and abietane derivatives are inhibitors of pyruvate dehydrogenase kinase (PDK) activity. The oxime 12 and dehydroabietyl amine 2 exhibit a blood glucose lowering effect in the diabetic ob/ob mouse after a single oral dose of 100 micromol/kg. However, the mechanism ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aicher TD,Damon RE,Koletar J,Vinluan CC,Brand LJ,Gao J,Shetty SS,Kaplan EL,Mann WR

更新日期：1999-08-02 00:00:00