Structural and functional insight of New Delhi Metallo β-lactamase-1 variants.

abstract：:An α-carbonic anhydrases (CAs, EC 4.2.1.1) was recently discovered, cloned and characterized in the genome of the protozoan parasite Trypanosoma cruzi, the causative agent of Chagas disease, a neglected but widespread tropical disease. Inhibition of this α-CAs (TcCA) with anions, sulfonamides, sulfamates, thiols and h...

journal_title：Future medicinal chemistry

authors： Supuran CT

更新日期：2016-01-01 00:00:00

abstract：:Chronic obstructive pulmonary disease (COPD) is one of the leading causes of death in the world today. Bronchodilators, particularly muscarinic antagonists and β(2) agonists, are recommended for patients with moderate to severe COPD. Dual-pharmacology muscarinic antagonist- β(2) agonist (MABA) molecules present an exc...

journal_title：Future medicinal chemistry

authors： Hughes AD,Jones LH

更新日期：2011-10-01 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：:The current state of antimalarial drug resistance emphasizes the need for new therapies with novel modes of action that will add a significant benefit compared with current standards. In this regard, high throughput phenotypic whole-cell screening aids the discovery of novel antiplasmodial scaffolds that are inherentl...

journal_title：Future medicinal chemistry

authors： Paquet T,Gordon R,Waterson D,Witty MJ,Chibale K

更新日期：2012-12-01 00:00:00

abstract：:Nicotinic receptors are membrane proteins involved in several physiological processes. They are considered suitable drug targets for various CNS disorders or conditions, as shown by the large number of compounds which have entered clinical trials. In recent years, nonconventional agonists have been discovered: positiv...

journal_title：Future medicinal chemistry

authors： Manetti D,Bellucci C,Chiaramonte N,Dei S,Teodori E,Romanelli MN

更新日期：2018-02-01 00:00:00

abstract：:Metal complexes have been the subject of numerous investigations in oncology but, despite the plethora of newly synthesized compounds, their precise mechanisms of action remain generally unknown or, for the best, incompletely determined. The continuous development of efficient and sensitive techniques in analytical ch...

journal_title：Future medicinal chemistry

authors： Marloye M,Berger G,Gelbcke M,Dufrasne F

更新日期：2016-12-01 00:00:00

abstract：:Trichomonas vaginalis and Entamoeba histolytica are clinically important protozoa that affect humans. T. vaginalis produces sexually transmitted infections and E. histolytica is the causative agent of amebic dysentery. Metronidazole, a compound first used to treat T. vaginalis in 1959, is still the main drug used worl...

journal_title：Future medicinal chemistry

authors： Moya IA,Su Z,Honek JF

更新日期：2009-07-01 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：: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：:Glioblastoma multiforme (GBM) is the most common primary malignant brain tumor in adults, associated with a high mortality rate and a survival of between 12 and 15 months after diagnosis. Due to current treatment limitations involving surgery, radiotherapy and chemotherapy with temozolamide, there is a high rate of tr...

journal_title：Future medicinal chemistry

authors： Ortiz R,Cabeza L,Perazzoli G,Jimenez-Lopez J,García-Pinel B,Melguizo C,Prados J

更新日期：2019-09-01 00:00:00

abstract：AIM:The assumption in scaffold hopping is that changing the scaffold does not change the binding mode and the same structure-activity relationships (SARs) are seen for substituents decorating each scaffold. Results/methodology: We present the use of matched series analysis, an extension of matched molecular pair analys...

journal_title：Future medicinal chemistry

authors： Hunt P,Segall M,O'Boyle N,Sayle R

更新日期：2017-01-01 00:00:00

abstract：:Aim: Anticancer immunochemotherapy represents an attractive paradigm to improve therapeutic responses and reduce side effects. Results & methodology: Here, we show that a naturally occurring host defense peptide, HN-1 inhibited multiple malignant cells proliferation and tumor growth in a xenografted human breast tumor...

journal_title：Future medicinal chemistry

authors： Qiao X,Yang H,Gao J,Cai S,Shi N,Wang M,Wang Y,Yu H

更新日期：2019-10-01 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：:Prodrug entrapment into nanocarriers for tumor delivery is a strategy to achieve a valid therapy with high efficiency. The prodrug contains anticancer agents conjugating with functional moieties or ligands so that the active component is released after metabolism in the body or tumor. The advantages of nanosystems for...

journal_title：Future medicinal chemistry

authors： Lin MH,Hung CF,Hsu CY,Lin ZC,Fang JY

更新日期：2019-08-01 00:00:00

abstract：:Platinum-based anticancer agents have been widely used in the clinic to successfully treat many different types of cancer. However, the therapeutic efficacy of platinum drugs is limited by serious side effects and the occurrence of inherent or acquired resistance of tumor cells. Nanoparticulate drug-delivery systems h...

journal_title：Future medicinal chemistry

authors： Bryde S,de Kroon AI

更新日期：2009-11-01 00:00:00

abstract：AIM:Triterpenes are natural compounds, whose wide biological activity predestines them for application as promising new chemotherapeutics. In this paper, we report the results of our investigations into the substitution of oleanolic acid with aromatic and nitroaromatic moieties acting as bioreducing agents. RESULTS:Th...

journal_title：Future medicinal chemistry

authors： Bednarczyk-Cwynar B,Ruszkowski P,Jarosz T,Krukiewicz K

更新日期：2018-03-01 00:00:00

abstract：:Filamenting temperature-sensitive mutant Z (FtsZ), an essential cell division protein in bacteria, has recently emerged as an important and exploitable antibacterial target. Cytokinesis in bacteria is regulated by the assembly dynamics of this protein, which is ubiquitously present in eubacteria. The perturbation of F...

journal_title：Future medicinal chemistry

authors： Panda D,Bhattacharya D,Gao QH,Oza PM,Lin HY,Hawkins B,Hibbs DE,Groundwater PW

更新日期：2016-06-01 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：: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: Angiotensin II receptor blockers were designed as therapeutic agents to block the binding site of the angiotensin II receptor type 1 (AT1R). Methodology: The structure of telmisartan was modified by coordination to the biometal Zn(II), resulting in the compound ZnTelm. Its antihypertensive activity and cel...

journal_title：Future medicinal chemistry

authors： Martínez VR,Aguirre MV,Todaro JS,Lima AM,Stergiopulos N,Ferrer EG,Williams PA

更新日期：2021-01-01 00:00:00

abstract：:Chi-Chao Chan, an American board certified ophthalmologist, is the Chief of Immunopathology Section, Laboratory of Immunology and the Head of Histology Core at the National Eye Institute at National Institutes of Health (USA). In 1967, Dr Chan graduated from Chungzhan Medical College in Guangzhou, China and then earne...

journal_title：Future medicinal chemistry

authors： Chan CC

更新日期：2012-11-01 00:00:00

abstract：:The DNA repair protein, O6-methylguanine DNA methyltransferase (MGMT), can confer resistance to guanine O6-alkylating agents. Therefore, inhibition of resistant MGMT protein is a practical approach to increase the anticancer effects of such alkylating agents. Numerous small molecule inhibitors were synthesized and exh...

journal_title：Future medicinal chemistry

authors： Sun G,Zhao L,Zhong R,Peng Y

更新日期：2018-08-01 00:00:00

abstract：:Aim: The explosion of data based technology has accelerated pattern mining. However, it is clear that quality and bias of data impacts all machine learning and modeling. Results & methodology: A technique is presented for using the distribution of first significant digits of medicinal chemistry features: logP, logS, a...

journal_title：Future medicinal chemistry

authors： García-Sosa AT

更新日期：2019-09-01 00:00:00

abstract：AIM:The present study was carried out to assess a new series of triazoloquinazolines 1-40 for their antioxidant activities using 1,1-diphenyl-2-picryl hydrazyl radical scavenging, ferric reduction antioxidant power and reducing power capability assays. RESULTS:All triazoloquinazolines 1-40 exhibited antioxidant activi...

journal_title：Future medicinal chemistry

authors： Al-Salahi R,Anouar EH,Marzouk M,Taie HA,Abuelizz HA

更新日期：2018-02-01 00:00:00

abstract：:More research effort needs to be invested in antimicrobial drug development to address the increasing threat of multidrug-resistant organisms. The enzyme DHPS has been a validated drug target for over 70 years as the target for the highly successful sulfa drugs. The use of sulfa drugs has been compromised by the wides...

journal_title：Future medicinal chemistry

authors： Hammoudeh DI,Zhao Y,White SW,Lee RE

更新日期：2013-07-01 00:00:00

abstract：:At present, the polysaccharide antitumor research is focused on how to further improve the antitumor activity of polysaccharides. The structural modification of polysaccharides can enhance their antitumor activity to a certain extent. The antitumor mechanisms of polysaccharide derivatives mainly contain the inducing a...

journal_title：Future medicinal chemistry

authors： Huang G,Huang H

更新日期：2017-10-01 00:00:00

abstract：:Aim: To synthesize novel antiproliferative agents. Results & methodology: A variety of 1,4-pentadien-3-one derivatives bearing quinoxaline scaffolds was designed and synthesized and their antiproliferative activities were evaluated. Notably, compounds N3 and N4 exhibited markedly greater antiproliferative activities a...

journal_title：Future medicinal chemistry

authors： Tang X,He J,Li Q,Tang X,Chen M,Hao G,Huai Z,Huang Y,Xue W

更新日期：2020-08-01 00:00:00

abstract：:In comparison with other virus infections, such as HIV, HBV, HCV, influenza and herpes virus, dengue virus infections have received relatively little attention from a (chemo)therapeutic viewpoint, despite their global incidence (2.5 billion people estimated to be at risk) and absence of an effective prophylactic measu...

journal_title：Future medicinal chemistry

authors： De Clercq E

更新日期：2010-04-01 00:00:00

abstract：:VEGF is an important signaling protein involved in both vasculogenesis and angiogenesis. As an essential receptor protein tyrosine kinase propagating cellular signal transduction processes, VEGFR-2 is a central target for drug discovery against tumor-associated angiogenesis. Since the autophosphorylation of VEGFR-2 re...

journal_title：Future medicinal chemistry

authors： Huang L,Huang Z,Bai Z,Xie R,Sun L,Lin K

更新日期：2012-09-01 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