Synthesis and dopamine transporter affinity of chiral 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines as potential cocaine abuse therapeutic agents.

abstract：:A 70% EtOH extract from the bark of Syringareticulata has shown significant antioxidant activity. Chemical study on the extract resulted in the isolation of seventeen compounds (1-17), including a novel oleoside-type secoiridoid glucoside, reticuloside (1), and the structures were elucidated on the basis of extensive ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bi X,Li W,Sasaki T,Li Q,Mitsuhata N,Asada Y,Zhang Q,Koike K

更新日期：2011-11-01 00:00:00

abstract：:A series of steroid-polyamine conjugates were synthesized and evaluated for their antimicrobial activity. This study was focused on the effect of stereochemistry at the C-3 and C-5 of steroids and types of polyamine at C-3 on activity against various human pathogens. All the conjugates exhibited strong antimicrobial a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim HS,Khan SN,Jadhav JR,Jeong JW,Jung K,Kwak JH

更新日期：2011-07-01 00:00:00

abstract：:The synthesis of a series of novel 1-[(benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles is described. The compounds were tested for human placental aromatase inhibition in vitro, using [1beta-3H]-androstenedione as the substrate for the aromatase enzyme, the percentage inhibition and IC50 data is included. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vinh TK,Ahmadi M,Delgado PO,Perez SF,Walters HM,Smith HJ,Nicholls PJ,Simons C

更新日期：1999-07-19 00:00:00

abstract：:(S)-4-(Carboxamido)phenylalanine (Cpa) is examined as a bioisosteric replacement for the terminal tyrosine (Tyr) residue in a variety of known peptide ligands for the mu, delta and kappa opioid receptors. The Cpa-containing peptides, assayed against cloned human opioid receptors, display comparable binding affinity (K...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dolle RE,Machaut M,Martinez-Teipel B,Belanger S,Cassel JA,Stabley GJ,Graczyk TM,DeHaven RN

更新日期：2004-07-05 00:00:00

abstract：:HER2 overexpression is associated with aggressive breast cancer with high recurrence rate and poor patient prognosis. Treatment of HER2 overexpressing patients with the HER2 targeting therapy trastuzumab results in acquired resistance within a year. The HER2/EGFR dual kinase inhibitor lapatinib was shown to inhibit so...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sridhar J,Sfondouris ME,Bratton MR,Nguyen TL,Townley I,Klein Stevens CL,Jones FE

更新日期：2014-01-01 00:00:00

abstract：:Crambescin B carboxylic acid, a synthetic analog of crambescin B, was recently found to inhibit the voltage-sensitive sodium channels (VSSC) in a cell-based assay using neuroblastoma Neuro 2A cells. In the present study, whole-cell patch-clamp recordings were conducted with three heterologously expressed VSSC subtypes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tsukamoto T,Chiba Y,Nakazaki A,Ishikawa Y,Nakane Y,Cho Y,Yotsu-Yamashita M,Nishikawa T,Wakamori M,Konoki K

更新日期：2017-03-01 00:00:00

abstract：:Fourty-two thiazolyl-pyrazoline derivatives were synthesized to screen for their EGFR kinase inhibitory activity. Compound 4-(4-chlorophenyl)-2-(3-(3,4-dimethylphenyl)-5-p-tolyl-4,5-dihydro-1H-pyrazol-1-yl)thiazole (11) displayed the most potent EGFR TK inhibitory activity with IC(50) of 0.06 μM, which was comparable ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lv PC,Li DD,Li QS,Lu X,Xiao ZP,Zhu HL

更新日期：2011-09-15 00:00:00

abstract：:We recently described a new family of bioactive molecules with interesting anti-cancer activities: the N-(4-(3-aminophenyl)thiazol-2-yl)acetamides. The lead compound of the series (1) displays significant anti-proliferative and cytotoxic activities against a panel of cancer cell lines, either sensitive or resistant to...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ronco C,Millet A,Plaisant M,Abbe P,Hamouda-Tekaya N,Rocchi S,Benhida R

更新日期：2017-05-15 00:00:00

abstract：:Hippuristanol is a natural product that has recently been shown to inhibit eukaryotic translation initiation and tumor cell proliferation. To investigate the structure and activity relationship of hippuristanol, we synthesized a series of analogs by expanding the size of its F ring and determined their effects on the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li W,Dang Y,Liu JO,Yu B

更新日期：2010-05-15 00:00:00

abstract：:Tryptamine derivatives, non-planar and potentially less toxic analogues of the anti-cancer agent fascaplysin, have been synthesised. They specifically inhibit Cdk4-D1 vis a vis Cdk2-A but, unlike fascaplysin, do not bind or intercalate DNA. CA224 is the most potent compound identified (Cdk4-D1 IC(50) approximately 5.5...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mahale S,Aubry C,James Wilson A,Jenkins PR,Maréchal JD,Sutcliffe MJ,Chaudhuri B

更新日期：2006-08-15 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：:A series of 4-aryl-2-(N-ethylanilino)pyrimidines has been synthesized as corticotropin-releasing hormone (CRH) inhibitors. The effect of substitution on each aromatic ring on receptor binding was investigated. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cocuzza AJ,Hobbs FW,Arnold CR,Chidester DR,Yarem JA,Culp S,Fitzgerald L,Gilligan PJ

更新日期：1999-04-05 00:00:00

abstract：:The first silanediol inhibitor of thermolysin is reported, prepared by analogy with the Grobelny/Bartlett phosphinate inhibitor. A Cbz group on nitrogen proved to be unstable to the triflic acid mediated silanediol deprotection and was replaced with a dihydrocinnamoyl group. The silanediol was prepared in high purity ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim J,Glekas A,McN Sieburth S

更新日期：2002-12-16 00:00:00

abstract：:Two new γ-lactones, aspergilactones A (1) and B (2), were discovered along with two known compounds, annularin A (3) and pericoterpenoid A (4), from a culture of the sponge-associated fungus Aspergillus sp. LS45. The planar structures of 1-4 were characterized using comprehensive spectroscopic methods and comparison w...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang L,Ding L,Li X,Wang N,Yan Y,Yang M,Cui W,Benjamin Naman C,Cheng K,Zhang W,Zhang B,Jin H,He S

更新日期：2019-07-01 00:00:00

abstract：:Pyrrole-imidazole polyamides can be synthesized to target predetermined sequences of DNA with nanomolar affinity and high specificity, and have been shown to modulate gene transcription both in vitro and in vivo. To make polyamides more readily available to biological laboratories, we have developed a rapid solid-phas...

journal_title：Bioorganic & medicinal chemistry letters

authors： Krutzik PO,Chamberlin AR

更新日期：2002-08-19 00:00:00

abstract：:Here we report a novel class of peptides-d-diaminopropionic acids (Dap)-for gene delivery. These peptides have attractive properties for gene delivery, and the advantage that they can be easily manipulated in relation to their composition, abiding with tailored-design. We characterized the toxicological and biophysica...

journal_title：Bioorganic & medicinal chemistry letters

authors： Viola JR,Strömberg R,Simonson OE,Andaloussi SE,Smith CI,Murtola M

更新日期：2012-09-01 00:00:00

abstract：:The targeted delivery of taxoids, in the form of taxane-antibody immunoconjugates, requires the preparation of taxoids containing moieties suitable for their conjugation to monoclonal antibodies. A series of taxoids incorporating a disulfide-containing linker at various positions of the taxoid framework have been prep...

journal_title：Bioorganic & medicinal chemistry letters

authors： Miller ML,Roller EE,Wu X,Leece BA,Goldmacher VS,Chari RV,Ojima I

更新日期：2004-08-02 00:00:00

abstract：:A series of novel tetracyclic core-containing HCV NS5A inhibitors has been discovered. Incorporation of tetrahydropyran-substituted amino acid moiety improved their potency and yielded HCV NS5A inhibitors with a minimum potency shift from the GT1a strain compared to other genotypes and mutants. Compounds 53 and 54 sho...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yu W,Hu B,Zhong B,Hao J,Lei Z,Agrawal S,Rokosz L,Liu R,Chen S,Asante-Appiah E,Kozlowski JA

更新日期：2019-03-01 00:00:00

abstract：:We aimed to discover a novel type of transient receptor potential vanilloid 1 (TRPV1) antagonist because such antagonists are possible drug candidates for treating various disorders. We modified the structure of hit compound 7 (human TRPV1 IC50=411 nM) and converted its pyrrolidino group to a (hydroxyethyl)methylamino...

journal_title：Bioorganic & medicinal chemistry letters

authors： Takahashi E,Hirano N,Nagahara T,Yoshikawa S,Momen S,Yokokawa H,Hayashi R

更新日期：2013-06-01 00:00:00

abstract：:S1P(1) receptor driven lymphopenia has proven utility in the treatment of an array of autoimmune disease states. As a part of our efforts to develop potent and selective S1P(1) receptor agonists, we have identified a novel chemical series of 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acid S1P(1) r...

journal_title：Bioorganic & medicinal chemistry letters

authors： Buzard D,Han S,Thoresen L,Moody J,Lopez L,Kawasaki A,Schrader T,Sage C,Gao Y,Edwards J,Barden J,Thatte J,Fu L,Solomon M,Liu L,Al-Shamma H,Gatlin J,Le M,Xing C,Espinola S,Jones RM

更新日期：2011-10-01 00:00:00

abstract：:Starting from the known FXR agonist GW 4064 1a, a series of alternately 3,5-substituted isoxazoles was prepared. Several of these analogs were potent full FXR agonists. A subset of this series, with a tether between the isoxazole ring and the 3-position aryl substituent, were equipotent FXR agonists to GW 4064 1a, wit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bass JY,Caldwell RD,Caravella JA,Chen L,Creech KL,Deaton DN,Madauss KP,Marr HB,McFadyen RB,Miller AB,Parks DJ,Todd D,Williams SP,Wisely GB

更新日期：2009-06-01 00:00:00

abstract：:Multiple-targeted ligands can have certain advantages for the management of hypertension which has multiple controls. Molecules with dual bioactivities are available in literature for treating metabolic disorders like diabetes, hypertension and hypercholesterolemia. After scrutinizing the SAR of prazosin-type α1-block...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yadav MR,Naik PP,Gandhi HP,Chauhan BS,Giridhar R

更新日期：2013-07-01 00:00:00

abstract：:Beauveria bassiana AM278 and Absidia coerulea AM93 converted 8-prenylnaringenin (1) into two glycoside derivatives (7-O-β-D-glucopyranoside) (2) and 7-O-β-D-4'''-O-methylglucopyranoside) (3) in high yields in processes conducted in Saboraud medium. 8-Prenylnaringenin 7-O-β-D-4'''-O-methylglucopyranoside (3) is a new c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bartmańska A,Tronina T,Huszcza E

更新日期：2012-10-15 00:00:00

abstract：:A series of regioisomeric bis-fulleropyrrolidines bearing two ammonium groups have been synthesized and their activities against HIV-1 and HIV-2 have been evaluated. Two trans isomers have been endowed with interesting antiviral properties, confirming the importance of the relative positions of the substituent on the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Marchesan S,Da Ros T,Spalluto G,Balzarini J,Prato M

更新日期：2005-08-01 00:00:00

abstract：:A series of isoquinuclidine benzamides as glycine uptake inhibitors for the treatment of schizophrenia are described. Potency, lipophilicity, and intrinsic human microsomal clearance were parameters for optimization. Potency correlated with the nature of the ortho substituents of the benzamide ring, and reductions in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Varnes JG,Xiong H,Forst JM,Holmquist CR,Ernst GE,Frietze W,Dembofsky B,Andisik DW,Palmer WE,Hinkley L,Steelman GB,Wilkins DE,Tian G,Jonak G,Potts WM,Wang X,Brugel TA,Alhambra C,Wood MW,Veale CA,Albert JS

更新日期：2018-04-01 00:00:00

abstract：:Insulin-like growth factor receptor (IGF-1R) is a growth factor receptor tyrosine kinase that acts as a critical mediator of cell proliferation and survival. Inhibitors of this receptor are believed to provide a new target in cancer therapy. We previously reported an isoquinolinedione series of IGF-1R inhibitors. Now ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Miller LM,Mayer SC,Berger DM,Boschelli DH,Boschelli F,Di L,Du X,Dutia M,Floyd MB,Johnson M,Kenny CH,Krishnamurthy G,Moy F,Petusky S,Tkach D,Torres N,Wu B,Xu W

更新日期：2009-01-01 00:00:00

abstract：:A novel series of potent zwitterionic uracil GnRH antagonists were discovered that showed reduced liability for CYP3A4 enzyme inhibition. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Regan CF,Guo Z,Chen Y,Huang CQ,Chen M,Jiang W,Rueter JK,Coon T,Chen C,Saunders J,Brown MS,Betz SF,Struthers RS,Yang C,Wen J,Madan A,Zhu YF

更新日期：2008-08-15 00:00:00

abstract：:A new series of quinoline ether inhibitors, which potently and selectively inhibit PDGFR tyrosine kinases, is described in this Letter. Compounds 23 and 33 are selective, low nanomolar inhibitors of PDGFRα and β, display good pharmacokinetics in rat and dog and are active in vivo at low doses when given orally twice d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Plé PA,Jung F,Ashton S,Hennequin L,Laine R,Lambert-van der Brempt C,Morgentin R,Pasquet G,Taylor S

更新日期：2012-05-01 00:00:00

abstract：:Derivatives of a CYP1A2 inhibitor rutaecarpine were synthesized to have potent and selective inhibition of human CYP1 members. Structural modelling shows a good fitting of rutaecarpine with the putative active site of human CYP1A2. Among the derivatives, 10- and 11-methoxyrutaecarpine are the most selective CYP1B1 inh...

journal_title：Bioorganic & medicinal chemistry letters

authors： Don MJ,Lewis DF,Wang SY,Tsai MW,Ueng YF

更新日期：2003-08-04 00:00:00

abstract：:A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives were synthesized via converting the readily available 4-hydroxy coumarin to the corresponding ethyl 2-(2-oxo-2H-chromen-4-yloxy)propanoate followed by hydrolysis and then reacting with different substituted amines. The molecular struct...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rambabu D,Mulakayala N,Ismail,Kumar KR,Kumar GP,Mulakayala C,Kumar CS,Kalle AM,Rao MV,Oruganti S,Pal M

更新日期：2012-11-01 00:00:00