Abstract:
:ABC, it's easy as 1 2 3! Bioisosteric replacement of the anilide core by an indole moiety considerably increased stability and gave potent and selective ABCG2 (BCRP) inhibitors. Some compounds are superior to the reference substances fumitremorgin C and Ko143 in terms of potency and efficacy and are the most potent ABCG2 modulators reported so far.
journal_name
ChemMedChemjournal_title
ChemMedChemauthors
Bauer S,Ochoa-Puentes C,Sun Q,Bause M,Bernhardt G,König B,Buschauer Adoi
10.1002/cmdc.201300319subject
Has Abstractpub_date
2013-11-01 00:00:00pages
1773-8issue
11eissn
1860-7179issn
1860-7187journal_volume
8pub_type
杂志文章相关文献
ChemMedChem文献大全abstract::Despite bioavailability issues, tea catechins have emerged as promising chemopreventive agents because of their efficacy in various animal models. We synthesized two catechin-derived compounds, 3-O-(3,4,5-trimethoxybenzoyl)-(-)-catechin (TMCG) and 3-O-(3,4,5-trimethoxybenzoyl)-(-)-epicatechin (TMECG), in an attempt to...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201000482
更新日期:2011-03-07 00:00:00
abstract::P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) is a major obstacle for successful cancer chemotherapy. Based on our previous study, 17 novel compounds with the 6,7-dimethoxy-2-{2-[4-(1H-1,2,3-triazol-1-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinoline scaffold were designed and synthesized. Among them, 2-[(1-...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201402463
更新日期:2015-02-01 00:00:00
abstract::PH-797804 ((aS)-3-{3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl}-N,4-dimethylbenzamde) is a diarylpyridinone inhibitor of p38 mitogen-activated protein (MAP) kinase derived from a racemic mixture as the more potent atropisomer (aS), first proposed by molecular modeling and subsequently confirmed ...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201100439
更新日期:2012-02-06 00:00:00
abstract::The histamine H1 G protein-coupled receptor (GPCR) plays an important role in allergy and inflammation. Existing drugs that address the H1 receptor differ in their chemical structure, pharmacology, and side effects. Light-controllable spatial and temporal activity regulation of photochromic H1 ligands may contribute t...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201800815
更新日期:2019-03-22 00:00:00
abstract::The asymmetric synthesis and receptor pharmacology of (1S,2R,3R,5R,6S)-2-amino-3-Hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (+)-9 (HYDIA) and a few of its O-alkylated derivatives are described. The key step of the synthesis utilizes Sharpless' asymmetric dihydroxylation (AD-beta) for the kinetic resolution of ...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.200700226
更新日期:2008-02-01 00:00:00
abstract::Cellular chaperones that belong to the heat-shock protein 90 (Hsp90) family are a prerequisite for successful viral propagation for most viruses. The hepatitis C virus (HCV) uses Hsp90 for maturation, folding, and modification of viral proteins. Based on our previous discovery that marine alkaloid analogues with a 4,5...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201800724
更新日期:2019-02-05 00:00:00
abstract::Better control of postprandial hyperglycemia can be achieved by delaying the absorption of glucose resulting from carbohydrate digestion. Because α-amylase initiates the hydrolysis of polysaccharides, the design of α-amylase inhibitors can lead to the development of new treatments for metabolic disorders such as type ...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201600427
更新日期:2016-11-07 00:00:00
abstract::A diverse group of proteins, the activities of which are precisely orchestrated during mitosis, have emerged as targets for cancer therapeutics; these include the Aurora kinases (AKs), Polo-like kinases (PLKs), and the kinesin spindle protein (KSP). KSP is essential for the proper separation of spindle poles during mi...
journal_title:ChemMedChem
pub_type: 杂志文章,评审
doi:10.1002/cmdc.201300228
更新日期:2013-11-01 00:00:00
abstract::The histone deacetylase (HDAC) family is a promising drug target class owing to the importance of these enzymes in a variety of cellular processes. Docking studies were conducted to identify novel HDAC inhibitors. Subtle modifications in the recognition domain were introduced into a series of chlamydocin analogues, an...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201300372
更新日期:2014-03-01 00:00:00
abstract::The serotonin transporter (SERT) is one of the neurotransmitter transporters that plays a critical role in the regulation of endogenous amine concentrations and therefore is an important target for therapeutic agents affecting the central nervous system. The recently published, high resolution X-ray structure of the c...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.200600242
更新日期:2007-06-01 00:00:00
abstract::DNA hypomethylating drugs that act on DNA methyltransferase (DNMT) isoforms are promising anticancer agents. By using a well-characterized live-cell system to measure DNA methylation revisions (imprints), we characterize olsalazine, an approved anti-inflammatory drug, as a novel DNA hypomethylating agent. The cell-bas...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201300555
更新日期:2014-03-01 00:00:00
abstract::A DNA-encoded chemical library (DECL) with 1.2 million compounds was synthesized by combinatorial reaction of seven central scaffolds with two sets of 343×492 building blocks. Library screening by affinity capture revealed that for some target proteins, the chemical nature of building blocks dominated the selection re...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201800193
更新日期:2018-07-06 00:00:00
abstract::The spider polyamine toxins Joro spider toxin-3 (JSTX-3) and Nephila polyamine toxins-1 and -8 (NPTX-1 and NPTX-8) are isolated from the venom of the orb-weaver spider Nephila clavata (Joro spider). They share a high degree of structural resemblance, their aromatic head groups being the only difference, and were recen...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201402278
更新日期:2014-12-01 00:00:00
abstract::A severe limitation in cancer therapy is the often insufficient differentiation between malign and benign tissue using known chemotherapeutics. One approach to decrease side effects is antibody-directed enzyme prodrug therapy (ADEPT). We have developed new glycosidic prodrugs such as (-)-(1S)-26 b based on the antibio...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.200800250
更新日期:2008-12-01 00:00:00
abstract::Disturbances of neutrotransmission at the dopamine D3 receptor are related to several neuropsychiatric diseases and in particular to drug addiction. Herein, we report the computer-assisted prediction of D3 selectivities of new fluoroalkoxy-substituted receptor ligands by means of 3D-QSAR analysis. As close analogues o...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.200700327
更新日期:2008-05-01 00:00:00
abstract::Protein tyrosine phosphatase 1B (PTP1B) is an important target for the treatment of diabetes. A series of thiazolidin-4-one derivatives 8-22 was designed, synthesized and investigated as PTP1B inhibitors. The new molecules inhibited PTP1B with IC50 values in the micromolar range. 5-(Furan-2-ylmethylene)-2-(4-nitrophen...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.202000055
更新日期:2020-07-03 00:00:00
abstract::Deoxyuridine 5'-triphosphate nucleotidohydrolase (dUTPase) is a potential drug target for malaria. We previously reported some 5'-tritylated deoxyuridine analogues (both cyclic and acyclic) as selective inhibitors of the Plasmodium falciparum dUTPase. Modelling studies indicated that it might be possible to replace th...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201100255
更新日期:2011-10-04 00:00:00
abstract::A series of 1,3,3,4-tetrasubstituted pyrrolidine containing CCR5 receptor antagonists were designed, which were elaborated either by condensation of a lithium salt of 3-(N,N-dibenzyl)aminopropionic acid methyl ester with ethyl benzoformate or by Baylis-Hillman reaction of ethyl acrylate with ethyl benzoformate and sub...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.200600182
更新日期:2007-02-01 00:00:00
abstract::The polyether ionophore salinomycin (SAL) has captured much interest because of its potent activity against cancer cells and cancer stem cells. Our previous studies have indicated that C1/C20 double-modification of SAL is a useful strategy to generate diverse agents with promising biological activity profiles. Thus, h...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201900593
更新日期:2020-01-17 00:00:00
abstract::Three photoswitchable tetrapeptides, based on a known synthetic antibacterial, were designed and synthesized to determine activity against Staphylococcus aureus. Each peptide contains an azobenzene photoswitch incorporated into either the N-terminal side chain (1), C-terminal side chain (2), or the C-terminus (3) to a...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.202000280
更新日期:2020-08-19 00:00:00
abstract::The in silico design, synthesis, and biological evaluation of ten potent type II dehydroquinase inhibitors are described. These compounds contain an anhydroquinate core, incorporated as a mimic of the enolate reaction intermediate. This substructure is attached by a variety of linking units to a terminal phenyl group ...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.200700032
更新日期:2007-07-01 00:00:00
abstract::With the widespread occurrence of bacterial resistance to antibiotics, the development of new strategies beyond conventional treatments is a pursuit taken by public health institutions worldwide. LasR, a transcription factor that controls quorum sensing in Pseudomonas aeruginosa, has emerged as an attractive therapeut...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201200434
更新日期:2013-01-01 00:00:00
abstract::This paper describes the synthesis, characterisation, and cytotoxicity of a novel trinuclear platinum complex code named TH1. In addition to its activity against human ovarian cancer cell lines: A2780, A2780(cisR), and A2780(ZD0473R), cell uptake, DNA-binding, and the nature of the compound interaction with pBR322 pla...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.200700204
更新日期:2008-01-01 00:00:00
abstract::Steroid derivatives bearing fluorescent groups such as anthracene, dansyl, deazaflavin, and pyrene attached to C6 were synthesized. These compounds are unique inhibitors of cytochrome P450 3A4 (CYP3A4) and display similar IC(50) values in the microM range for the CYP3A4 substrates midazolam, testosterone, and nifedipi...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.200600300
更新日期:2007-05-01 00:00:00
abstract::Aberrant WNT pathway activation, leading to nuclear accumulation of β-catenin, is a key oncogenic driver event. Mutations in the tumor suppressor gene APC lead to impaired proteasomal degradation of β-catenin and subsequent nuclear translocation. Restoring cellular degradation of β-catenin represents a potential thera...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.202000839
更新日期:2020-12-04 00:00:00
abstract::Targeting protein-protein interactions, such as the HIV-1 gp120-CD4 interface, has become a cutting-edge approach in the current drug discovery scenario. Many small molecules have been developed so far as inhibitors of the interaction between CD4 and HIV-1 gp120. However, due to a variety of reasons such as solubility...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201200584
更新日期:2013-03-01 00:00:00
abstract::Selective inhibitors of the protein tyrosine phosphatase SHP2 (src homology region 2 domain phosphatase; PTPN11), an enzyme that is deregulated in numerous human tumors, were generated through a combination of chemical synthesis and structure-based rational design. Seventy pyridazolon-4-ylidenehydrazinyl benzenesulfon...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201500015
更新日期:2015-05-01 00:00:00
abstract::Loperamide (1a), an opioid receptor agonist, is in clinical use as an antidiarrheal agent. Carbon/silicon exchange (sila-substitution) at the 4-position of the piperidine ring of 1a (R3 COH→R3 SiOH) leads to sila-loperamide (1b). Sila-loperamide was synthesized in a multistep procedure, starting from triethoxyvinylsil...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201500040
更新日期:2015-05-01 00:00:00
abstract::A series of water-soluble (benzoyloxy)methyl esters of acetylsalicylic acid (ASA), commonly known as aspirin, are described. The new derivatives each have alkyl chains containing a nitric oxide (NO)-releasing nitrooxy group and a solubilizing moiety bonded to the benzoyl ring. The compounds were synthesized and evalua...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201300105
更新日期:2013-07-01 00:00:00
abstract::Intraoperative imaging technologies recently entered the operating room, and their implementation is revolutionizing how physicians plan, monitor, and perform surgical interventions. In this work, we present a novel surgical imaging reporter system: intraoperative chemiluminescence imaging (ICI). To this end, we have ...
journal_title:ChemMedChem
pub_type: 杂志文章
doi:10.1002/cmdc.201600301
更新日期:2016-09-20 00:00:00