AzaHx, a novel fluorescent, DNA minor groove and G·C recognition element: Synthesis and DNA binding properties of a p-anisyl-4-aza-benzimidazole-pyrrole-imidazole (azaHx-PI) polyamide.

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：:Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites. In order to reduce attrition due to metabolism-induced toxicity and to improve the safety of drug candidates, we developed a simple cell viability assay by combining a bioactivation system (huma...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rana P,Will Y,Nadanaciva S,Jones LH

更新日期：2016-08-15 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：:Several benzocyclobutacarbazol derivatives were synthesized and evaluated for their potential cytotoxic properties. A number of these compounds exhibited significant antiproliferative activity with concomitant interaction with the cell cycle and represent a new class of potential anticancer agents. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Graf-Christophe S,Kuehm-Caubère C,Renard P,Pfeiffer B,Pierré A,Léonce S,Caubère P

更新日期：2000-12-04 00:00:00

abstract：:A novel cosalane analog having an extended polyanionic pharmacophore was synthesized in order to target specific cationic residues on the surface of CD4. The design rationale is based on a hypothetical binding model of cosalane to the surface of the protein. The new analog displayed an EC50 of 0.55 microM as an inhibi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cushman M,Insaf S,Ruell JA,Schaeffer CA,Rice WG

更新日期：1998-04-07 00:00:00

abstract：:Positioning of reactive functional groups within a DNA duplex can enable chemical reactions that otherwise would not occur to an appreciable extent. However, few studies have quantitatively defined the extent to which the enforced proximity of reaction partners in duplex DNA can favor chemical processes. Here, we meas...

journal_title：Bioorganic & medicinal chemistry letters

authors： Catalano MJ,Price NE,Gates KS

更新日期：2016-06-01 00:00:00

abstract：:The synthesis of a 20 member 2-aminoimidazole/triazole pilot library is reported. Each member of the library was screened for its ability to inhibit or promote biofilm development of either Escherichia coli and Acinetobacter baumannii. From this screen, E. coli-selective 2-aminoimidazoles were discovered, with the bes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Reed CS,Huigens RW 3rd,Rogers SA,Melander C

更新日期：2010-11-01 00:00:00

abstract：:The search for new antimicrobial agents is greater than ever due to the perpetual threat of multidrug resistance in known pathogens and the relentless emergence of new infections. In this manuscript, ten thiazole-based thiazolidinone hybrids bearing a 6-trifluoromethoxy substituent on the benzothiazole core were synth...

journal_title：Bioorganic & medicinal chemistry letters

authors： Haroun M,Tratrat C,Petrou A,Geronikaki A,Ivanov M,Ciric A,Sokovic M

更新日期：2021-01-15 00:00:00

abstract：:Rhus verniciflua Stokes has been used as a traditional herbal medicine in Asia. In this study, the effect of R. verniciflua extract on human aromatase (cytochrome P450 19, CYP19) activity was investigated to elucidate the mechanism for the effect of R. verniciflua extract on androgen hormone levels. Androstenedione wa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park MH,Kim IS,Kim SA,Na CS,Hong CY,Dong MS,Yoo HH

更新日期：2014-04-01 00:00:00

abstract：:Seedlings of natural crops are valuable sources of pharmacologically active phytochemicals. In this study, we aimed to identify new active secondary metabolites in Avena sativa L. (oat) seedlings. Two new compounds, avenafuranol (1) and diosgenoside (2), along with eight known compounds (3-10) were isolated from the A...

journal_title：Bioorganic & medicinal chemistry letters

authors： Woo SY,Lee KS,Shin HL,Kim SH,Lee MJ,Young Kim H,Ham H,Lee DJ,Choi SW,Seo WD

更新日期：2020-07-15 00:00:00

abstract：:A series of 3-chloro-4-substituted-1-(8-hydroxy-quinolin-5-yl)-azetidin-2-ones were synthesized and evaluated for their in vitro anti-filarial activity. To pre-assess the anti-filarial behavior of synthesized compounds (V(a-f)) on a structural basis, automated docking studies were carried out with Molecular Design Sui...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chhajed SS,Manisha P,Bastikar VA,Animeshchandra H,Ingle VN,Upasani CD,Wazalwar SS

更新日期：2010-06-15 00:00:00

abstract：:A novel series of oxadiazole EP1 receptor antagonists was identified by replacing the amide of a known glycine sulfonamide derivative with a 1,3,4-oxadiazole. Optimization of the substitution patterns on the three aromatic rings led to the identification of high affinity EP1 receptor antagonists. The derivative with h...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hall A,Brown SH,Chowdhury A,Giblin GM,Gibson M,Healy MP,Livermore DG,Wilson RJ,Naylor A,Rawlings DA,Roman S,Ward E,Willay C

更新日期：2007-08-15 00:00:00

abstract：:The acyloxyalkyl derivatives of a model anti-HBV dinucleotide were synthesized and evaluated as orally bioavailable prodrugs. Our studies have led to the identification of the first orally bioavailable dinucleotide prodrugs for further therapeutic development against the hepatitis B virus (HBV). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Coughlin JE,Padmanabhan S,Zhang G,Kirk CJ,Govardhan CP,Korba BE,O'Loughlin K,Green CE,Mirsalis J,Morrey JD,Iyer RP

更新日期：2010-03-01 00:00:00

abstract：:Cyclic phosphatidic acid (CPA) is a naturally occurring analog of lysophosphatidic acid (LPA) in which the sn-2 hydroxy group forms a five-membered ring with the sn-3 phosphate. Here, we describe the synthesis of R-3-CCPA and S-3-CCPA along with their pharmacological properties as inhibitors of lysophospholipase D/aut...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gupte R,Siddam A,Lu Y,Li W,Fujiwara Y,Panupinthu N,Pham TC,Baker DL,Parrill AL,Gotoh M,Murakami-Murofushi K,Kobayashi S,Mills GB,Tigyi G,Miller DD

更新日期：2010-12-15 00:00:00

abstract：:4,4-dimethyl-5 alpha-cholesta-8,14,24-trien-3 beta-ol, a sterol of current biological interest, has been synthesized in six steps from 3 beta-acetoxy-4,4-dimethyl-5 alpha-cholest-8(14)-en-15-one. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ruan B,Wilson WK,Schroepfer GJ Jr

更新日期：1998-02-03 00:00:00

abstract：:The stereochemical effects of the hydrocarbon crosslink on the conformation and cellular uptake of i,i+4 stapled peptides were studied. Compared to its S,S-configurated counterpart, the crosslink bearing the R,R-configuration provided a significantly diminished helix stabilizing effect and conferred less efficient cel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim YW,Verdine GL

更新日期：2009-05-01 00:00:00

abstract：:A range of amphiphilic sorbitan ethers has been synthesized in two steps from sorbitan following an acetalization/hydrogenolysis sequence. These sorbitan ethers and the acetal intermediates have been evaluated as antimicrobials against Gram-negative and Gram-positive bacteria. No antimicrobial activity was observed fo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Belmessieri D,Gozlan C,Duclos MC,Dumitrescu O,Lina G,Redl A,Duguet N,Lemaire M

更新日期：2017-10-15 00:00:00

abstract：:SB-216763 is a novel, potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor with an IC(50) value of 34 nM. [(11)C]SB-216763 (3-(2,4-dichlorophenyl)-4-(1-[(11)C]methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione), a new potential PET agent for imaging of GSK-3, was first designed and synthesized in 20-30% decay cor...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang M,Gao M,Miller KD,Sledge GW,Hutchins GD,Zheng QH

更新日期：2011-01-01 00:00:00

abstract：:Low-temperature NMR experiments and molecular modeling have been used to characterize the conformational behavior of a covalently cross-linked DNA base pair model. The data suggest that Watson-Crick or reverse Watson-Crick hydrogen bonding geometries have similar energies and can interconvert at low temperatures. This...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jensen EA,Allen BD,Kishi Y,O'Leary DJ

更新日期：2008-11-15 00:00:00

abstract：:Two new C(29) sterols with a cyclopropane ring at C-25 and C-26, petrosterol-3,6-dione (1) and 5alpha,6alpha-epoxy-petrosterol (2), along with petrosterol (3), were isolated from the Vietnamese marine sponge Ianthella sp. The structures of the new compounds were elucidated by comprehensive spectroscopic analyses. Comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nguyen HT,Chau VM,Tran TH,Phan VK,Hoang TH,Nguyen TD,Nguyen XN,Tai BH,Hyun JH,Kang HK,Kim YH

更新日期：2009-08-15 00:00:00

abstract：:A convenient and efficient palladium-catalysed retro-ene-assisted method has been developed to prepare a series of 5-substituted-6-phenyl-3(2H)-pyridazinones as potential antiplatelet drugs. The most active compounds were those that contain a 3-phenyl-3-oxo-propenyl fragment or a phenylthio group at position 5 of the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Coelho A,Sotelo E,Fraiz N,Yáñez M,Laguna R,Cano E,Raviña E

更新日期：2004-01-19 00:00:00

abstract：:A kinetic analysis of an enzyme assay employing a synthetic substrate that produces a detectable signal through a spontaneous organic cyclization/elimination reaction following the enzymatic reaction was conducted. The results from the calculation were used to predict the lag period and provide accurate measurements o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xue F,Seto CT

更新日期：2011-02-01 00:00:00

abstract：:We describe herein a novel series of 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective inhibitors against the CXCR2 chemokine receptor and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Furthermore, these alkyl-hydrazine series inhibitors such as 5b demonstrated acceptable metabolic stab...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu S,Liu Y,Wang H,Ding Y,Wu H,Dong J,Wong A,Chen SH,Li G,Chan M,Sawyer N,Gervais FG,Henault M,Kargman S,Bedard LL,Han Y,Friesen R,Lobell RB,Stout DM

更新日期：2009-10-01 00:00:00

abstract：:Pimavanserin is a selective serotonin 2A receptor (5-HT2AR) inverse agonist that has shown promise for treatment of psychotic symptoms in patients with Parkinson's disease. Here, we detail the (11)C-labeling and subsequently evaluate pimavanserin as a PET-radioligand in pigs. [(11)C]Pimavanserin was obtained by N-meth...

journal_title：Bioorganic & medicinal chemistry letters

authors： Andersen VL,Hansen HD,Herth MM,Dyssegaard A,Knudsen GM,Kristensen JL

更新日期：2015-03-01 00:00:00

abstract：:A new class of benzimidazole-5-sulfonamides has been identified as nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Initial structure-activity relationships are presented resulting in compounds 19 and 28 with submicromolar dual functional activity on human and rat receptors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hashimoto K,Tatsuta M,Kataoka M,Yasoshima K,Shogase Y,Shimazaki M,Yura T,Li Y,Yamamoto N,Gupta JB,Urbahns K

更新日期：2005-02-01 00:00:00

abstract：:A series of m-carborane derivatives was prepared based upon the structures of antiestrogenic drugs and their activities were evaluated by estrogen receptor alpha (ERalpha) binding assay and transactivation assay using human breast cancer cell line, MCF-7 cells. The m-carborane bisphenol 5 exhibited about a thousand ti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ogawa T,Ohta K,Yoshimi T,Yamazaki H,Suzuki T,Ohta S,Endo Y

更新日期：2006-08-01 00:00:00

abstract：:A series of new peptoids as endothelin receptor antagonists has been synthesized. Screening them for their ability to bind with endothelin receptors (ET(A) and ET(B)) competitively in the presence of (125I) endothelin led to the discovery of compounds as possible leads with IC50s in the low micromolar concentrations. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dasgupta F,Gangadhar N,Bruhaspathy M,Verma AK,Sarin S,Mukherjee AK

更新日期：2001-02-26 00:00:00

abstract：:Two (99m)Tc/Re complexes based on flavone and aurone were tested as potential probes for imaging β-amyloid plaques using single photon emission computed tomography. Both (99m)Tc-labeled derivatives showed higher affinity for Aβ(1-42) aggregates than did (99m)Tc-BAT. In sections of brain tissue from an animal model of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ono M,Ikeoka R,Watanabe H,Kimura H,Fuchigami T,Haratake M,Saji H,Nakayama M

更新日期：2010-10-01 00:00:00

abstract：:The recent success of vemurafenib shows the importance of selective BRAF V600E inhibition in melanoma. However, paradoxical activation by structurally diverse ATP-competitive RAF kinase inhibitors strongly suggests that selective CRAF inhibitors, not BRAF inhibitors, would be ideal for some Ras mutation cancer treatme...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aman W,Lee J,Kim M,Yang S,Jung H,Hah JM

更新日期：2016-02-15 00:00:00

abstract：:Heterocyclic amide isosteres were incorporated into a phenylglycine-based tissue factor/factor VIIa (TF-FVIIa) inhibitor chemotype, providing potent inhibitors. An X-ray co-crystal structure of phenylimidazole 19 suggested that an imidazole nitrogen atom effectively mimics an amide carbonyl, while the phenyl ring form...

journal_title：Bioorganic & medicinal chemistry letters

authors： Glunz PW,Cheng X,Cheney DL,Weigelt CA,Wei A,Luettgen JM,Wong PC,Wexler RR,Priestley ES

更新日期：2015-01-01 00:00:00