解剖学和形态学
麻醉学
听力与言语-语言病理学
行为科学
心脏和心血管系统
细胞和组织工程学
临床神经病学
危重症监护医学
牙科,口腔外科和医学
皮肤病学
急诊医学
内分泌学和新陈代谢
肠胃学和肝脏学
老人病学和老年医学
卫生保健科学和服务
血液学
免疫学
传染病
综合和补充性医学
医学伦理学
医学信息学
医学实验室技术
医学,全科和内科
医学,法律
医学,研究和试验
神经系统科学
护理
营养学和饮食学
产科医学和妇科医学
肿瘤学
眼科学
整形外科学
耳鼻喉科学
病理学
儿科学
周围血管疾病
药理学和药剂学
生理学
基本医疗保健
精神病学
公共、环境和职业卫生
放射学,核医学和医学成像
康复学
生殖生物学
呼吸系统
风湿病学
运动科学
外科学
毒理学
热带医学
泌尿学和肾脏学
病毒学
老年医学
健康政策和服务
心理学,临床
abstract::Radiopharmaceuticals are localized in (malignant) tumor tissues by different mechanisms. One of these mechanisms, gelatinase enzyme activity, is associated with poor prognosis in cancer patients and potential targets for tumor imaging. There are some gelatinases to be associated with metastatic potential for tumor ima...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12253
更新日期:2014-03-01 00:00:00
abstract::In this research, a series of substituted 5-(5-amino-1-aryl-1H-pyrazol-4-yl)-1H-tetrazoles were synthesized and evaluated for in vitro antileishmanial activity. Among the derivatives, examined compounds 3b and 3l exhibited promising activity against promastigotes and amastigotes forms of Leishmania amazonensis. The cy...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12235
更新日期:2014-03-01 00:00:00
abstract::The development of isozyme-selective carbonic anhydrase inhibitors is currently still a great challenge. In the present study, protein-ligand complex structures were obtained by AutoDock Vina with SBR ((R)-N-(3-indol-1-yl-2-methyl-propyl)-4-sulfamoyl-benzamide) as the only inhibitor docked into the binding pockets of ...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12234
更新日期:2014-02-01 00:00:00
abstract::HIV-1 integrase enzyme plays an important role in the life cycle of HIV and responsible for integration of virus into human genome. Here, both computational and synthetic approaches were used to design and synthesize newer HIV-1 integrase inhibitors. Pharmacophore mapping was performed on 20 chemically diverse molecul...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12207
更新日期:2014-02-01 00:00:00
abstract::Novel, potent non-imidazole histamine H3 receptor antagonists have been prepared and in vitro tested as H3 -receptor antagonists (the electrically evoked contraction of the guinea-pig jejunum). The present compounds contain a 4-hydroxypiperidine core, which behaves as a conformationally restricted version of the 3-ami...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12206
更新日期:2014-01-01 00:00:00
abstract::The NS5B RNA-dependent RNA polymerase (RdRP) is a promising therapeutic target for developing novel anti-hepatitis C virus (HCV) drugs. In this work, a combined molecular modeling study was performed on a series of 193 5-hydroxy-2H-pyridazin-3-one derivatives as inhibitors of HCV NS5B Polymerase. The best 3D-QSAR mode...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12203
更新日期:2014-01-01 00:00:00
abstract::Phosphodiesterase 11 (PDE11) is the latest isoform of the PDEs family to be identified, acting on both cyclic adenosine monophosphate and cyclic guanosine monophosphate. The initial reports of PDE11 found evidence for PDE11 expression in skeletal muscle, prostate, testis, and salivary glands; however, the tissue distr...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12193
更新日期:2013-12-01 00:00:00
abstract::Methoxy-substituted chalcones, 3 were obtained using simple, efficient method from 2-naphtylethanone, 1 and aromatic aldehydes, 2. The in vitro cytotoxicity activities of the chalcones against a panel of three human cancer cell lines were explored. The tested compounds were found to possess significant cytotoxic activ...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12184
更新日期:2013-12-01 00:00:00
abstract::Frequency of tuberculosis is progressively increasing worldwide. New emerging strains of bacilli that are emerging are resistant to the currently available drugs which make this issue more alarming. In this regard, a series of substituted quinolinyl chalcones, quinolinyl pyrimidines, and pyridines were synthesized and...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12178
更新日期:2013-12-01 00:00:00
abstract::The first example of an inhibitor of the kinase TAK1 that binds in the DFG-out conformation is disclosed. These preliminary studies used kinase-targeted screening and structure-based drug design to create a molecule with dual pharmacological inhibition of p38 and TAK1 that demonstrated significant activity in a cell-b...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12169
更新日期:2013-11-01 00:00:00
abstract::Benzimidazole and their metal analogs that can act as multimodal agent and have non-peptidic CCK-B receptor antagonist were synthesized and characterized on the basis of spectroscopic techniques such as FT-IR, NMR, FAB-MS and also evaluated for biologic efficacy. The ligands showed binding to most of the organs, known...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12201
更新日期:2013-11-01 00:00:00
abstract::During SAR development of previously reported pyrrolocarbazole 1, a potent PARP-1 inhibitor, compound 14, was discovered serendipitously to be a prodrug of compound 1. ...
journal_title:Chemical biology & drug design
pub_type: 信件
doi:10.1111/cbdd.12165
更新日期:2013-09-01 00:00:00
abstract::Alyteserin-2a (ILGKLLSTAAGLLSNL.NH2 ) stimulated the rate of insulin release from BRIN-BD11 clonalβ cells at a concentration of 30 nm (p < 0.05) with a response of 296 ± 26% of basal release at 3 μm (p < 0.001). The insulinotropic actions of analogs containing substitutions by l-lysine, d-lysine, or l-tryptophan at si...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12151
更新日期:2013-08-01 00:00:00
abstract::A novel series of 5-(2-alkyl/aryl-6-arylimidazo[2,1-b][1,3,4]thiadiazol-5-yl)methylene-1,3-thiazolidinediones were synthesized as possible PPARγ agonists. The structures of these target molecules were established by spectral and analytical data. All the newly synthesized compounds were screened for their in vivo hypog...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12140
更新日期:2013-08-01 00:00:00
abstract::Follicle-stimulating hormone is important for mammalian reproduction. It acts through specific receptors located on the plasma membrane of granulosa cells in ovaries and Sertoli cells in testes. The binding of follicle-stimulating hormone to its receptor activates intracytoplasmic signaling pathways leading to steroid...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12149
更新日期:2013-08-01 00:00:00
abstract::The flavonoid baicalein has been proven effective in animal models of parkinson's disease; however, the potential biological targets and molecular mechanisms underlying the antiparkinsonian action of baicalein have not been fully clarified. In the present study, the potential targets of baicalein were predicted by in ...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12127
更新日期:2013-06-01 00:00:00
abstract::New imines, derived from aromatic aldehyde, chalcones and 5-amino-1,3,4-thiadiazole-2-thiol exhibited promising anti-convulsant activity which is explained through chemo-biological interactions at receptor site producing the inhibition of human Carbonic Anhydrase-II enzyme (hCA-II) through the proposed pharmacophore m...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12113
更新日期:2013-05-01 00:00:00
abstract::Two series of [1,2,4]triazolo[3,4-a]phthalazine and tetrazolo[5,1-a]phthalazine derivatives bearing substituted benzylpiperazine moieties have been synthesized and evaluated for their positive inotropic activity by measuring left atrium stroke volume on isolated rabbit heart preparations. The majority of the derivativ...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12101
更新日期:2013-05-01 00:00:00
abstract::Epstein-Barr virus (EBV) infects more than 90% of the world population. Following primary infection, Epstein-Barr virus persists in an asymptomatic latent state. Occasionally, it may switch to lytic infection. Latent EBV infection has been associated with several diseases, such as Burkitt lymphoma (BL). To date, there...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12109
更新日期:2013-05-01 00:00:00
abstract::Malfunction or overexpression of ErbB receptors (epidermal growth factor receptors) is associated with occurrence and severity of several types of cancer. Initiation of signal cascades by ErbB2 (also known as human epidermal growth factor receptor 2/neu) in breast cancer has been blocked by monoclonal antibodies such ...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12062
更新日期:2013-04-01 00:00:00
abstract::The relevance of CB(2)-mediated therapeutics is well established in the treatment of pain, neurodegenerative and gastrointestinal tract disorders. Recent works such as the crystallization of class-A G-protein-coupled receptors in a range of active states and the identification of specific anchoring sites for CB(2) ago...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12095
更新日期:2013-04-01 00:00:00
abstract::Polyazamacrocycles are currently being studied and used in a variety of applications beyond their traditional place in supramolecular and co-ordination chemistry. This study suggests additional applications of these compounds with particular emphasis on their use as antiproliferative agents that could be potentially u...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12098
更新日期:2013-04-01 00:00:00
abstract::Utilizing atypical wake-promoting agent modafinil (inactive in both rH(3) and hH(3) binding assays) as a launching pad, a series of sulfinyl- and sulfone-derived H(3) receptor inverse agonists were developed. Brain-permeable compound 27, a potent member of the series displayed excellent selectivity against related fam...
journal_title:Chemical biology & drug design
pub_type: 信件
doi:10.1111/cbdd.12094
更新日期:2013-03-01 00:00:00
abstract::Selective blockade of the serotonin 5-HT(2A) receptor is a useful therapeutic approach for a number of disorders, including schizophrenia, insomnia and ischaemic heart disease. A series of aporphines were docked into a homology model of the rat 5-HT(2A) receptor using AutoDock. Selected compounds with high in silico b...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12069
更新日期:2013-02-01 00:00:00
abstract::A series of thiouracil derivatives were designed, synthesized and screened for in vitro inhibition of dipeptidyl peptidase IV. The SAR study indicated the influence of substituted chemical modifications on thiouracil scaffold. Compounds 8 (IC(50) = 0.32 μM), 9 (IC(50) = 0.29 μM), and 12 (IC(50) = 0.25 μM) showed excel...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12070
更新日期:2013-02-01 00:00:00
abstract::We report the first account of a comparative analysis of the binding affinities of nine FDA-approved drugs against subtype B as well as the South African subtype C HIV PR (C-SA). A standardized protocol was used to generate the inhibitor/C-SA PR complexes with the relative positions of the inhibitors taken from the co...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12063
更新日期:2013-02-01 00:00:00
abstract::Protein flexibility plays a major role in biomolecular recognition. In many cases, it is not obvious how molecular structure will change upon association with other molecules. In proteins, these changes can be major, with large deviations in overall backbone structure, or they can be more subtle as in a side-chain rot...
journal_title:Chemical biology & drug design
pub_type: 杂志文章,评审
doi:10.1111/cbdd.12051
更新日期:2013-01-01 00:00:00
abstract::As protein/protein interactions usually trigger signalling processes, inhibitors of those interactions must preclude protein binding without eliciting the signalling process themselves. To accomplish those goals, small molecules need to target those protein residues that contribute the most to binding (binding hotspot...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12075
更新日期:2013-01-01 00:00:00
abstract::Unprotected S-acylated cysteine isopeptides containing α-, β- or γ-amino acid units have been synthesized, and their conversion to native hexapeptides by S- to the N-terminus ligations involving 17-, 18- and 19-membered cyclic transition states have been demonstrated both experimentally and computationally to be more ...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12053
更新日期:2012-12-01 00:00:00
abstract::The screening of an in-house quinolones library against Mycobacterium tuberculosis (Mtb) H(37) Rv, followed by a first cycle of optimization, yielded 6-hydrogen-8-methyl derivatives endowed with good potency. The antitubercular activity also encompassed the bacteria in a non-replicating state (NRP-TB) with minimum inh...
journal_title:Chemical biology & drug design
pub_type: 信件
doi:10.1111/cbdd.12022
更新日期:2012-11-01 00:00:00
abstract::Peroxisome-proliferator-activated receptors are a class of nuclear receptors with three subtypes: α, γ and δ. Their main function is regulating gene transcription related to lipid and carbohydrate metabolism. Currently, there are no peroxisome-proliferator-activated receptors δ drugs being marketed. In this work, we s...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2012.01424.x
更新日期:2012-10-01 00:00:00
abstract::During the past century, several epidemics of human African trypanosomiasis, a deadly disease caused by the protist Trypanosoma brucei, have afflicted sub-Saharan Africa. Over 10 000 new victims are reported each year, with hundreds of thousands more at risk. As current drug treatments are either highly toxic or ineff...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2012.01392.x
更新日期:2012-08-01 00:00:00
abstract::The chemokines and their receptors play a key role in immune and inflammatory responses by promoting recruitment and activation of different subpopulations of leukocytes. The membrane receptor CXCR3 binds three chemokines, CXCL9, CXCL10, and CXCL11, and its involvement is recognized in many inflammatory diseases and c...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2012.01397.x
更新日期:2012-08-01 00:00:00
abstract::The present study describes ligand-based pharmacophore modeling of a series of structurally diverse acyl coenzyme A cholesterol acyltransferase inhibitors. Quantitative pharmacophore models were generated using HypoGen module of Discovery Studio 2.1, whereby the best pharmacophore model possessing two hydrophobic, one...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2012.01384.x
更新日期:2012-07-01 00:00:00
abstract::A cholesteryl-functionalized derivative of activity dependent neurotrophic factor-9 peptide (a nine amino acid core peptide of activity-dependent neurotrophic factor, acting against Alzheimer's disease) was synthesized aiming at the improvement of its bioavailability. Therefore, its uptake was comparatively investigat...
journal_title:Chemical biology & drug design
pub_type: 信件
doi:10.1111/j.1747-0285.2012.01381.x
更新日期:2012-07-01 00:00:00
abstract::Six lycorine derivatives were prepared, characterized, and evaluated for their in vitro anti-Trichomonas vaginalis activity. Compounds bearing an acetyl (2), lauroyl (3), benzoyl (4 and 5), and p-nitrobenzoyl (6 and 7) groups were synthesized. The best activity was achieved with lycorine esterified at C-2 position wit...
journal_title:Chemical biology & drug design
pub_type: 信件
doi:10.1111/j.1747-0285.2012.01333.x
更新日期:2012-07-01 00:00:00
abstract::Structure-activity relationship (SAR) studies are essential in the generation of peptides with enhanced activity and efficacy as therapeutic agents. In this study, we report a Structure-activity relationship study for a family of mimetic peptides derived from type IV collagen with potent anti-angiogenic properties. Th...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2012.01376.x
更新日期:2012-07-01 00:00:00
abstract::Forty-eight chromone derivatives were evaluated for their antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl free radical scavenging assay, ferrous ions (Fe(2+) ) chelating activity test, total antioxidant activity test (Ferric thiocyanate and Thiobarbituric acid methods), and total reductive capability (potassi...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2012.01368.x
更新日期:2012-06-01 00:00:00
abstract::Tuberculosis is the second leading infectious killer with 9 million new cases in 2009. Extensive use of pathogen's lipid metabolism especially in utilizing the host lipids and virulence highlights the importance of exported lipid-catabolizing enzymes. Current study aims to emphasize the importance of Rv0183, an export...
journal_title:Chemical biology & drug design
pub_type: 信件
doi:10.1111/j.1747-0285.2012.01373.x
更新日期:2012-06-01 00:00:00
abstract::To understand the protein transduction domain (PTD)-mediated protein transduction behavior and to explore its potential in delivering biopharmaceutic drugs, we prepared four TAT-EGFP conjugates: TAT(+)-EGFP, TAT(-)-EGFP, EGFP-TAT(+) and EGFP-TAT(-), where TAT(+) and TAT(-) represent the original and the reversed TAT s...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2011.01315.x
更新日期:2012-05-01 00:00:00