N3-substituted thymidine bioconjugates for cancer therapy and imaging.

abstract：:Several hundred genes associated or linked to obesity have been described in the scientific literature. Whereas many of these genes are potential targets for the treatment of obesity and associated conditions, none of them have permitted the developement of an efficient drug therapy. As proposed by the 'thrifty genoty...

journal_title：Future medicinal chemistry

authors： Braud S,Ciufolini M,Harosh I

更新日期：2010-12-01 00:00:00

abstract：:Sialic acid is associated with glycoproteins and gangliosides of eukaryotic cells. It regulates various molecular interactions, being implicated in inflammation and cancer, where its expression is regulated by sialyltransferases and sialidases. Angiogenesis, the formation of new capillaries, takes place during inflamm...

journal_title：Future medicinal chemistry

authors： Chiodelli P,Urbinati C,Paiardi G,Monti E,Rusnati M

更新日期：2018-12-01 00:00:00

abstract：BACKGROUND:Benzimidazole derivatives are promising compounds for the treatment of parasitic infections. The structure-activity relationships of 91 benzimidazoles with activity against Trichomonas vaginalis and Giardia intestinalis were analyzed using a novel activity landscape modeling approach. RESULTS:We identified ...

journal_title：Future medicinal chemistry

authors： Aguayo-Ortiz R,Pérez-Villanueva J,Hernández-Campos A,Castillo R,Meurice N,Medina-Franco JL

更新日期：2014-03-01 00:00:00

abstract：:Since the Hedgehog signaling pathway has been associated with cancer, it has emerged as a therapeutic target for cancer therapy. The main target among the key Hedgehog proteins is the GPCR-like Smo receptor. Therefore, some Smo antagonists that have entered clinical trials, including the US FDA-approved drugs vismodeg...

journal_title：Future medicinal chemistry

authors： Espinosa-Bustos C,Mella J,Soto-Delgado J,Salas CO

更新日期：2019-03-01 00:00:00

abstract：:This review summarizes the basic milestones of the research of 5-azacytosine nucleosides chronologically from their discovery and anticancer activity identification, through to subsequent unveiling of their mechanism of action based on DNA hypomethylation and tumor-suppressor gene reactivation, to the final US FDA app...

journal_title：Future medicinal chemistry

authors： Krečmerová M,Otmar M

更新日期：2012-05-01 00:00:00

abstract：:Camellia oleifera Abel is a member of Camellia, and its seeds are used to extract Camellia oil, which is generally used as cooking oil in the south of China. Camellia oil consists of unsaturated fatty acids, tea polyphenol, squalene, saponin, carrot element and vitamins, etc. The seed remains after oil extraction of C...

journal_title：Future medicinal chemistry

authors： Xiao X,He L,Chen Y,Wu L,Wang L,Liu Z

更新日期：2017-11-01 00:00:00

abstract：:Structure-based virtual screening makes explicit or implicit use of 3D target structure information to detect novel active compounds. Results of nearly 300 currently available original applications have been analyzed to characterize the state-of-the-art in this field. Compound selection from docking calculations is mu...

journal_title：Future medicinal chemistry

authors： Ripphausen P,Stumpfe D,Bajorath J

更新日期：2012-04-01 00:00:00

abstract：AIM:Cisplatin resistance in ovarian cancer remains a complex problem as tumors frequently develop resistance against drugs, a mechanism sometimes mediated by ATP-Binding Cassette transporters. Our goal was to find compounds restricting their inhibition capacity to the cisplatin efflux mediated by ABCC2 pump, among prev...

journal_title：Future medicinal chemistry

authors： Comsa E,Nguyen KA,Loghin F,Boumendjel A,Peuchmaur M,Andrieu T,Falson P

更新日期：2018-06-01 00:00:00

abstract：:Systematic investigation of the lipidome will reveal new opportunities for disease diagnosis and intervention. However, lipidomic research has been hampered by the lack of molecular tools to track specific lipids of interest. Accumulating reports indicate lipid recognition can be achieved with properly constructed sho...

journal_title：Future medicinal chemistry

authors： Gao J,Zheng H

更新日期：2013-05-01 00:00:00

abstract：AIM:The design and synthesis of chromenopyrimidines as microtubule destabilizing agents. MATERIALS & METHODS:Novel chromenopyrimidines and chromenotriazolopyrimidines were prepared and evaluated for their cytotoxicity against MCF-7 cell line. The most potent compound was tested for its possible effect on tubulin inhib...

journal_title：Future medicinal chemistry

authors： El-Bakhshawangy NM,El-Nassan HB,Kassab AE,Taher AT

更新日期：2018-06-01 00:00:00

abstract：:Due to the impermeable structure and barrier function of the blood-brain barrier (BBB), the delivery of therapeutic molecules into the CNS is extremely limited. Nanodelivery systems are regarded as the most effective and versatile carriers for the CNS, as they can transport cargo molecules across the BBB via various m...

journal_title：Future medicinal chemistry

authors： Kim KT,Lee HS,Lee JJ,Park EK,Lee BS,Lee JY,Bae JS

更新日期：2018-11-01 00:00:00

abstract：:The use of electron density-based molecular descriptors in drug research, particularly in quantitative structure--activity relationships/quantitative structure--property relationships studies, is reviewed. The exposition starts by a discussion of molecular similarity and transferability in terms of the underlying elec...

journal_title：Future medicinal chemistry

authors： Matta CF,Arabi AA

更新日期：2011-06-01 00:00:00

abstract：:Since their initial isolation from the marine alga Delisea pulchra, bromofuranones have been investigated as potential inhibitors of quorum sensing (QS) in various bacterial strains. QS is an important mechanism by which bacteria co-ordinate their molecular response to the environment. QS is intrinsically linked to ba...

journal_title：Future medicinal chemistry

authors： Lyons T,Gahan CG,O'Sullivan TP

更新日期：2020-11-01 00:00:00

abstract：:New Delhi Metallo β-lactamase-1 (NDM-1) is a member of the Metallo-β-lactamase family, capable of catalyzing the hydrolysis of all β-lactam antibiotics. The rapid dissemination of NDM producers, 'superbugs', has become a worldwide concern to health workers. Seventeen different variants of NDM have been reported so far...

journal_title：Future medicinal chemistry

authors： Khan S,Ali A,Khan AU

更新日期：2018-01-01 00:00:00

abstract：:During the current decade, data on the post-translational hydroxylation of specific amino acid residues of some ribosomal proteins and translation factors in both eukaryotes and eubacteria have accumulated. The reaction is catalyzed by dedicated oxygenases (so-called ribosomal oxygenases), whose action is impaired und...

journal_title：Future medicinal chemistry

authors： Graifer D,Malygin A,Karpova G

更新日期：2019-02-25 00:00:00

abstract：:HIV/AIDS remains a formidable disease with millions of individuals inflicted worldwide. Although treatment regimens have improved considerably, drug resistance brought on by viral mutation continues to erode their effectiveness. Intense research efforts are currently underway in search of new and improved therapies. T...

journal_title：Future medicinal chemistry

authors： Ghosh AK,Anderson DD

更新日期：2011-07-01 00:00:00

abstract：:Although activity has been reported in vivo, free nucleic acid-based drugs are rapidly degraded and cleared following systemic administration. To address these challenges and improve the potency and bioavailability of genetic drugs, significant efforts have been made to develop effective delivery systems of which lipi...

journal_title：Future medicinal chemistry

authors： Lin PJ,Tam YK

更新日期：2015-01-01 00:00:00

abstract：:With the goal of refining our discovery DMPK workflow, we conducted a retrospective analysis on internal Celgene compounds by calculating the physicochemical properties and gathering data from several assays including solubility, rat and human liver S9 stability, Caco-2 permeability, and rat intravenous (iv.) and oral...

journal_title：Future medicinal chemistry

authors： Kulkarni A,Riggs J,Phan C,Bai A,Calabrese A,Shi T,Moghaddam MF

更新日期：2014-02-01 00:00:00

abstract：:Diabetes mellitus is an increasing public health problem in the world. Type 2 diabetes is the most common type of diabetes whose complications contribute to its high death rate. It seriously impacts healthcare systems and patients' quality of life. Therefore, effective measures and new treatment strategies are needed ...

journal_title：Future medicinal chemistry

authors： Turdu G,Gao H,Jiang Y,Kabas M

更新日期：2018-05-01 00:00:00

abstract：:The rise of antibiotic resistant bacteria requires unconventional strategies toward efficient chemotherapeutic agents, preferably with alternative mechanisms of action. The bacterial cell membrane has become an appealing target since its essential and highly conservative structure are key challenges to resistance mech...

journal_title：Future medicinal chemistry

authors： Dias C,Rauter AP

更新日期：2019-02-25 00:00:00

abstract：:Due to the unusual structure and chemical composition of the mycobacterial cell wall, effective tuberculosis (TB) treatment is difficult, making many antibiotics ineffective and hindering the entry of drugs. With approximately 33% of infection, TB is still the second most deadly infectious disease worldwide. The reaso...

journal_title：Future medicinal chemistry

authors： Chauhan PM,Sunduru N,Sharma M

更新日期：2010-09-01 00:00:00

abstract：:Immunoadjuvant Quillaja spp. tree saponins stimulate both cellular and humoral responses, significantly widening vaccine target pathogen spectra. Host toxicity of specific saponins, fractions and extracts may be rather low and further reduced using lipid-based delivery systems. Saponins contain a hydrophobic central a...

journal_title：Future medicinal chemistry

authors： Magedans YV,Yendo AC,Costa F,Gosmann G,Fett-Neto AG

更新日期：2019-06-01 00:00:00

abstract：AIM:Currently, dozens of BRAF inhibitors and MEK inhibitors targeting RAF-MEK-ERK pathway have been introduced into clinical trials for cancer therapy. However, after 6-8 months of initial response, acquired drug resistance among the majority of those treated patients sharply diminished their clinical efficacy. DISCUS...

journal_title：Future medicinal chemistry

authors： Yu Z,Ye S,Hu G,Lv M,Tu Z,Zhou K,Li Q

更新日期：2015-01-01 00:00:00

abstract：:Cancer is a major devastating disease, and is a leading cause of death worldwide. Despite the progress in cancer treatment, cancer mortality rate remains high. Therefore, the discovery and development of improved anticancer drugs to treat cancer are needed. 4H-chromenes have strong cytotoxicity against a panel of huma...

journal_title：Future medicinal chemistry

authors： Patil SA,Patil R,Pfeffer LM,Miller DD

更新日期：2013-09-01 00:00:00

abstract：:Despite the wealth of information available for the reverse transcriptase (RT)-associated ribonuclease H (RNaseH) domain of lentiviruses, gammaretroviruses and long terminal repeat containing retrotransposons, exploiting this information in the form of an RNaseH inhibitor with high specificity and low cellular toxicit...

journal_title：Future medicinal chemistry

authors： Corona A,Masaoka T,Tocco G,Tramontano E,Le Grice SF

更新日期：2013-12-01 00:00:00

abstract：AIM:Alzheimer's disease is a progressive and neurodegenerative disorder of the CNS, affecting elderly people. The current pharmacological approach is based on the improvement of cholinergic neurotransmission by inhibiting acetylcholinesterase (AChE) with AChE inhibitors. The disease is also characterized by the acceler...

journal_title：Future medicinal chemistry

authors： de Almeida JR,Figueiro M,Almeida WP,de Paula da Silva CHT

更新日期：2018-05-01 00:00:00

abstract：:Lysophosphatidic acid (LPA) and its receptors, LPA1-6, are integral parts of signaling pathways involved in cellular proliferation, migration and survival. These signaling pathways are of therapeutic interest for the treatment of multiple types of cancer and to reduce cancer metastasis and side effects. Validated ther...

journal_title：Future medicinal chemistry

authors： Parrill AL

更新日期：2014-05-01 00:00:00

abstract：:Bromodomain and extra-terminal domain (BET) protein family plays an important role in regulating gene transcription preferentially at super-enhancer regions and has been involved with several types of cancers as a candidate. Up to now, there are 16 pan-BET inhibitors in clinical trials, however, most of them have unde...

journal_title：Future medicinal chemistry

authors： Yang Y,Wu Z,Chen P,Zheng P,Zhang H,Zhou J

更新日期：2020-09-01 00:00:00

abstract：AIM:There is little information available on the monoamine oxidase isoform selectivity of N-alkyl harmine analogs, which exhibit a myriad of activities including MAO-A, DYRK1A and cytotoxicity to several select cancer cell lines. RESULTS:Compounds 3e and 4c exhibited an IC50 of 0.83 ± 0.03 and 0.43 ± 0.002 μM against ...

journal_title：Future medicinal chemistry

authors： Haider S,Alhusban M,Chaurasiya ND,Tekwani BL,Chittiboyina AG,Khan IA

更新日期：2018-06-01 00:00:00

abstract：:Micro-organisms express a wide range of transmembrane pumps known as multidrug efflux pumps that improve the micro-organism's ability to survive in severe environments and contribute to resistance against antibiotic and antimicrobial agents. There is significant interest in developing efflux inhibitors as an adjunct t...

journal_title：Future medicinal chemistry

authors： Jamshidi S,Sutton JM,Rahman KM

更新日期：2016-01-01 00:00:00