当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > The synthesis of amino-acid functionalized beta-carbolines as topoisomerase II inhibitors.

The synthesis of amino-acid functionalized beta-carbolines as topoisomerase II inhibitors.

Abstract：

:The synthesis and biological activity of amino acid functionalized beta-carboline derivatives, which are structurally related to azatoxin and the tryprostatins, are reported. These compounds were assayed for their growth inhibition properties in H520 and PC3 cell lines and were examined for their abilities to inhibit topoisomerase II-mediated DNA relaxation.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Deveau AM,Labroli MA,Dieckhaus CM,Barthen MT,Smith KS,Macdonald TL

doi

10.1016/s0960-894x(01)00136-6

subject

Has Abstract

pub_date

2001-05-21 00:00:00

pages

1251-5

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960894X01001366

journal_volume

11

pub_type

杂志文章

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Synthesis of [18F]SU11248, a new potential PET tracer for imaging cancer tyrosine kinase.

    abstract：:N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-[18F]fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, a new potential positron emission tomography tracer for imaging cancer tyrosine kinase, has been prepared by the nucleophilic substitution of the nitro-precursor N-[2-(diethylamino)ethyl]...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.06.038

    authors： Wang JQ,Miller KD,Sledge GW,Zheng QH

    更新日期：2005-10-01 00:00:00

  • Synthesis and biological evaluation of unnatural derivatives of narciclasine: 7-aza-nornarciclasine and its N-oxide.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.07.034

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

    更新日期：2014-09-01 00:00:00

  • Synthesis and thrombolytic activity of fibrinogen fragment related cyclopeptides.

    abstract：:In the modification of the fibrinogen fragment related sequences ARPAK, QRPAK GRPAK and KRPAK, the corresponding cyclo-ARPAK, cyclo-QRPAK, cyclo-GRPAK, and cyclo-KRPAK were prepared in the diluted solution. The bioassay in vivo indicated that the thrombolytic potencies of cyclo-ARPAK, cyclo-GRPAK, cyclo-QRPAK, and cyc...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)01072-7

    authors： Zhao M,Lin N,Wang C,Peng S

    更新日期：2003-03-10 00:00:00

  • Syntheses and antiproliferative evaluation of oxyphenisatin derivatives.

    abstract：:Syntheses and structure-antiproliferative relationship for oxyphenisatin analogues are described. The cell proliferation data showed that the presence of substituents (especially F, Cl, Me, CF(3), and OMe) in the 6- and 7-position of oxyphenisatin markedly enhanced the potency in the MDA-468 cell line without affectin...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2007.02.060

    authors： Uddin MK,Reignier SG,Coulter T,Montalbetti C,Grånäs C,Butcher S,Krog-Jensen C,Felding J

    更新日期：2007-05-15 00:00:00

  • Structure-activity relationships of untenone A and its derivatives for inhibition of DNA polymerases.

    abstract：:We found that untenone A and mannzamenone A inhibit mammalian DNA polymerases alpha and beta, and human terminal deoxynucleotidyl transferase (TdT). The syntheses of both compounds and the structure-activity relationships of untenone A derivatives are described. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.01.092

    authors： Saito F,Takeuchi R,Kamino T,Kuramochi K,Sugawara F,Sakaguchi K,Kobayashi S

    更新日期：2004-04-19 00:00:00

  • Synthesis and biological evaluation of novel heterocyclic quinones as inhibitors of the dual specificity protein phosphatase CDC25C.

    abstract：:A focused set of heterocyclic quinones based on the benzothiazole, benzoxazole, benzimidazole, indazole and isoindole was prepared and screened with respect to the inhibition of the phosphatase activity of CDC25C. Benzoxazole- and benzothiazole-diones were at least 50 times more potent in inhibiting CDC25C than their ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.09.030

    authors： Lavergne O,Fernandes AC,Bréhu L,Sidhu A,Brézak MC,Prévost G,Ducommun B,Contour-Galcera MO

    更新日期：2006-01-01 00:00:00

  • Synthesis, characterization and activity of new phosphonate dipeptides as potential inhibitors of VanX.

    abstract：:VanX, a Zn(II)-dependent D-ala-D-ala dipeptidase, is essential for vancomycin resistance in Enterococcus faecium. The enzymatic activity of VanX was previously found to be inhibited competitively by 2-{[(1-aminoethyl) (hydroxy) phosphoryl]oxy} propanoic acid (1B). Here we report the synthesis and characterization of s...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.10.094

    authors： Jia C,Yang KW,Liu CC,Feng L,Xiao JM,Zhou LS,Zhang YL

    更新日期：2012-01-01 00:00:00

  • Discovery of novel indazole-linked triazoles as antifungal agents.

    abstract：:The in vitro and in vivo activities of a series of (2R,3R)-2-(2,4-difluorophenyl)-3-(substituted indazol-1-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol as potential antifungal agents are described. In particular, the analog 12j having 5-bromo substitution on the indazole ring exhibited significant antifungal activity again...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2007.03.074

    authors： Park JS,Yu KA,Kang TH,Kim S,Suh YG

    更新日期：2007-06-15 00:00:00

  • Synthesis and biological evaluation of the pirfenidone derivatives as antifibrotic agents.

    abstract：:A total of 24 pirfenidone derivatives were designed, synthesized and evaluated for their inhibitory activity against the human lung fibroblast cell line MRC-5. These compounds showed the remarkable proliferation inhibition against MRC-5 compared to pirfenidone as the positive control. The possible mechanism of this ki...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.11.038

    authors： Ma Z,Pan Y,Huang W,Yang Y,Wang Z,Li Q,Zhao Y,Zhang X,Shen Z

    更新日期：2014-01-01 00:00:00

  • A combinatorial approach to chemical modification of subtilisin Bacillus lentus.

    abstract：:The reaction between methanethiosulfonate reagents and cysteine mutants of subtilisin is quantitative and can be used to prepare chemically modified mutant enzymes (CMMs) with novel properties. The virtually unrestricted structural variations possible for CMMs presents a preparative and screening challenge. To address...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(98)00415-6

    authors： Plettner E,Khumtaveeporn K,Shang X,Jones JB

    更新日期：1998-09-08 00:00:00

  • Synthesis and in vivo evaluation of 3,4-disubstituted gababutins.

    abstract：:A range of 3,4-alkylated five-membered ring derivatives of gabapentin were synthesised. One compound (21) had an excellent level of potency against alpha(2)delta and was profiled in in vivo models of pain and anxiety. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.10.121

    authors： Blakemore DC,Bryans JS,Carnell P,Field MJ,Kinsella N,Kinsora JK,Meltzer LT,Osborne SA,Thompson LR,Williams SC

    更新日期：2010-01-01 00:00:00

  • Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.

    abstract：:Three series of rhodanine derivatives bearing a quinoline moiety (6a-h, 7a-g, and 8a-e) have been synthesized, characterized, and evaluated as antibacterial agents. The majority of these compounds showed potent antibacterial activities against several different strains of Gram-positive bacteria, including multidrug-re...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.05.082

    authors： Guo M,Zheng CJ,Song MX,Wu Y,Sun LP,Li YJ,Liu Y,Piao HR

    更新日期：2013-08-01 00:00:00

  • Novel 12-membered non-antibiotic macrolides from erythromycin A; EM900 series as novel leads for anti-inflammatory and/or immunomodulatory agents.

    abstract：:Herein, we report the design and synthesis of the novel 12-membered non-antibiotic macrolide (8R,9S)-8,9-dihydro-6,9-epoxy-8,9-anhydropseudoerythromycin A (EM900), which was found to be a potent anti-inflammatory and/or immunomodulatory agent, capable of promoting monocyte to macrophage differentiation. This molecule ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.04.004

    authors： Sugawara A,Sueki A,Hirose T,Nagai K,Gouda H,Hirono S,Shima H,Akagawa KS,Omura S,Sunazuka T

    更新日期：2011-06-01 00:00:00

  • Isotope edited NMR studies of glycosidases: design and synthesis of a novel glycosidase inhibitor.

    abstract：:N-13C-methyl-deoxynojirimycin was synthesized and used in isotope-edited NMR studies to probe the binding site of an alpha-glucosidase. Results from this analysis led to the design and preparation of a novel alpha-glucosidase inhibitor, N-glycyl deoxynojirimycin. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00175-4

    authors： Hines JV,Chang H,Gerdeman MS,Warn DE

    更新日期：1999-05-03 00:00:00

  • Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent.

    abstract：:We report herein the synthesis of a newly described anti-cancer agent, NRPa-308. This compound antagonizes Neuropilin-1, a multi-partners transmembrane receptor overexpressed in numerous tumors, and thereby validated as promising target in oncology. The preparation of NRPa-308 proved challenging because of the orthogo...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.126710

    authors： Brachet E,Dumond A,Liu WQ,Fabre M,Selkti M,Raynaud F,Hermine O,Benhida R,Belmont P,Garbay C,Lepelletier Y,Ronco C,Pagès G,Demange L

    更新日期：2019-12-15 00:00:00

  • Inhibition of the ras-dependent mitogenic pathway by phosphopeptide prodrugs with antiproliferative properties.

    abstract：:Phosphopeptide prodrugs bearing two S-acyl-2-thioethyl (SATE) biolabile phosphate protections were developed. They are capable to inhibit the Shc/Grb2 interaction and MAP kinases (ERK1 and ERK2) phosphorylation in cellular assay. The S-acetyl-2-thioethyl (MeSATE) analogue showed an IC50 of 1 microM in the inhibition o...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00077-9

    authors： Liu WQ,Vidal M,Mathé C,Périgaud C,Garbay C

    更新日期：2000-04-03 00:00:00

  • Structure-activity relationship studies of novel 3-oxazolidinedione-6-naphthyl-2-pyridinones as potent and orally bioavailable EP3 receptor antagonists.

    abstract：:Multiple regions of the 3-oxazolidinedione-6-naphthyl-pyridinone series identified via high throughput screening were explored. SAR studies of these regions including the left-hand side oxazolidinedione moiety, α-substituent on the oxazolidinedione ring, central pyridinone core, and substituents on the central pyridin...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.03.107

    authors： Morales-Ramos ÁI,Li YH,Hilfiker M,Mecom JS,Eidam P,Shi D,Tseng PS,Brooks C,Zhang D,Wang N,Jaworski JP,Morrow D,Fries H,Edwards R,Jin J

    更新日期：2011-05-15 00:00:00

  • Synthesis and antitumor activity of s-tetrazine derivatives.

    abstract：:Fifty-five compounds of s-tetrazine derivative including hexahydro-, 1,6-dihydro, 1,4-dihydro-, 1,2-dihydro- and aromatic s-tetrazine were prepared. Their antitumor activities were evaluated in vitro by MTT method for P-388 cell and SRB method for A-549 cell. The results show that there are 9 compounds which in 10(-6)...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2003.12.056

    authors： Hu WX,Rao GW,Sun YQ

    更新日期：2004-03-08 00:00:00

  • Synthesis and protonation behavior of a water-soluble N-fused porphyrin: conjugation with an oligoarginine by click chemistry.

    abstract：:A water-soluble derivative of N-fused porphyrin (NFP) possessing a nona-arginine (R9) peptide tail was synthesized for the first time by a Cu(I)-catalyzed azide-alkyne 'click' reaction. In aqueous solution, at pH 8, the conjugated molecule (NFP-R9) exists as free base and protonated below pH<6.5 to form monoprotonated...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.03.066

    authors： Ikawa Y,Harada H,Toganoh M,Furuta H

    更新日期：2009-05-01 00:00:00

  • Design and regioselective synthesis of a new generation of targeted chemotherapeutics. Part II: Folic acid conjugates of tubulysins and their hydrazides.

    abstract：:Efficient syntheses of folate conjugates of tubulysins and their hydrazides 1a-d are described. These water soluble folate receptor (FR) targeted conjugates are derivatives of folic acid and the potent cytotoxic agents: tubulysin A, B, or their respective hydrazides, connected in regioselective manner via a hydrophili...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.07.041

    authors： Vlahov IR,Wang Y,Kleindl PJ,Leamon CP

    更新日期：2008-08-15 00:00:00

  • Design and characterization of non-phosphopeptide inhibitors for Src family SH2 domains.

    abstract：:The development of novel non-phosphopeptide inhibitors for the Src family SH2 domain is described. Several commercially available hydroxyl aromatic acids have been appended off the N-terminus of pYEEIE and the potent phosphopeptide inhibitors of GST-Lck-SH2 were identified via ELISA. The most potent inhibitor, caffeic...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00523-1

    authors： Park SH,Won J,Lee KH

    更新日期：2002-10-07 00:00:00

  • Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs.

    abstract：:Structure-based drug design was exploited in the synthesis of 3-(6-chloronaphth-2-ylsulfonyl)aminopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating an alanylamide P4 group with acyclic tertiary amide termini. Optimized hydrophobic contacts of one amide substituent in P4 were complemented by hydrophobici...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.09.001

    authors： Young RJ,Campbell M,Borthwick AD,Brown D,Burns-Kurtis CL,Chan C,Convery MA,Crowe MC,Dayal S,Diallo H,Kelly HA,King NP,Kleanthous S,Mason AM,Mordaunt JE,Patel C,Pateman AJ,Senger S,Shah GP,Smith PW,Watson NS,West

    更新日期：2006-12-01 00:00:00

  • Thiourea inhibitors of herpes viruses. Part 1: bis-(aryl)thiourea inhibitors of CMV.

    abstract：:Bis-(aryl)thioureas were found to be potent and selective inhibitors of cytomegalovirus (CMV) in cultured HFF cells. Of these, the thiazole analogue 38 was investigated as a potential development candidate. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(03)00586-9

    authors： Bloom JD,DiGrandi MJ,Dushin RG,Curran KJ,Ross AA,Norton EB,Terefenko E,Jones TR,Feld B,Lang SA

    更新日期：2003-09-01 00:00:00

  • Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives.

    abstract：:3-Azido-, 3-amino- and 3-(1,2,3-triazol-1-yl)-β-lactams were synthesized and evaluated for their antiplasmodial activity against four strains of Plasmodium falciparum and KB cells for their cytotoxicity profiles. The presence of a cyclohexyl substituent at N-1 and a phenyl group on the triazole ring markedly improved ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.05.119

    authors： Singh P,Sachdeva S,Raj R,Kumar V,Mahajan MP,Nasser S,Vivas L,Gut J,Rosenthal PJ,Feng TS,Chibale K

    更新日期：2011-08-01 00:00:00

  • Chemoselective enrichment as a tool to increase access to bioactive natural products: Case study borrelidin.

    abstract：:Chemoselective purification technologies have seen great success in biomolecule isolation, with a classic example being the genetically-encoded His tag utilized to enrich desired proteins from a crude lysate. We sought to translate this purification tactic into a powerful tool for the isolation of natural products and...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.07.062

    authors： Trader DJ,Carlson EE

    更新日期：2015-11-01 00:00:00

  • Discovery of 4-anilino-N-methylthieno[3,2-d]pyrimidines and 4-anilino-N-methylthieno[2,3-d]pyrimidines as potent apoptosis inducers.

    abstract：:We report the discovery of N-((benzo[d][1,3]dioxol-5-yl)methyl)-6-phenylthieno[3,2-d]pyrimidin-4-amine (2a) as an apoptosis inducer using our proprietary cell- and caspase-based ASAP HTS assay, and SAR study of HTS hit 2a which led to the discovery of 4-anilino-N-methylthieno[3,2-d]pyrimidines and 4-anilino-N-methylth...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.04.145

    authors： Kemnitzer W,Sirisoma N,May C,Tseng B,Drewe J,Cai SX

    更新日期：2009-07-01 00:00:00

  • Structural basis of the dynamic mechanism of ligand binding to cyclooxygenase.

    abstract：:Molecular modeling studies performed on the two cyclooxygenase (COX) isozymes suggest that the cavity at the mouth of the active site on the membrane domain that may act as an actual binding site of COX ligands. Actual docking of different inhibitors at this site provides a structural basis to explain the dynamics of ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00481-3

    authors： Llorens O,Perez JJ,Palomer A,Mauleon D

    更新日期：1999-10-04 00:00:00

  • Furans with basic side chains: synthesis and biological evaluation of a novel series of antagonists with selectivity for the estrogen receptor alpha.

    abstract：:3-alkyl-2,4,5-triarylfurans with basic side-chain substituents were prepared as ligands for the estrogen receptor. Those analogues having the basic side chain on the C(4) phenol were high-affinity, ERalpha-selective antagonists. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(01)00488-7

    authors： Mortensen DS,Rodriguez AL,Sun J,Katzenellenbogen BS,Katzenellenbogen JA

    更新日期：2001-09-17 00:00:00

  • Synthesis and evaluation of 3-¹²³I-iodo-5-[2-(S)-3-pyrrolinylmethoxy]-pyridine (niodene) as a potential nicotinic α4β2 receptor imaging agent.

    abstract：:Nicotinic acetylcholine receptors (nAChRs) are downregulated in disease conditions such as Alzheimer's and substance abuse. Presently, (123)I-5-IA-85380 is used in human studies and requires over 6h of scanning time, thus increases patient discomfort. We have designed and synthesized 3-iodo-5-[2-(S)-3-pyrrolinylmethox...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.10.012

    authors： Pandey SK,Pan S,Kant R,Kuruvilla SA,Pan ML,Mukherjee J

    更新日期：2012-12-15 00:00:00

  • Design and synthesis of 2-substituted benzoxazoles as novel PTP1B inhibitors.

    abstract：:A series of benzoxazole compounds containing oxamic acid were synthesized and screened for the PTP1B inhibition. Compound 31d showed best biochemical potency (Ki) of 6.7 μM. Structure-activity relationship were explained with the help of molecular modeling approach. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.02.109

    authors： Chandrasekharappa AP,Badiger SE,Dubey PK,Panigrahi SK,Manukonda SR

    更新日期：2013-05-01 00:00:00