Design, synthesis and biological activity of new polyenolic inhibitors of matrix metalloproteinases: a focus on chemically-modified curcumins.

abstract：BACKGROUND:Cancer metabolic reprogramming rekindles enthusiasm for the research of metabolic regulation in cancer drug resistance. A growing number of metabolic modifiers combined with cancer drugs obtain the expected efficacy in in vitro or in vivo studies, also in clinical trial studies, indicating a good potential o...

journal_title：Current medicinal chemistry

authors： Tan W,Zhong Z,Wang S,Liu H,Yu H,Tan R,Hu X,Pan T,Wang Y

更新日期：2017-11-17 00:00:00

abstract：:APN is an important zinc dependent metallo-exopeptidase; it has been considered as a suitable target for anti-cancer drug design. In this review we focus on the most effective and the most promising inhibitors of aminopeptidase N. Their binding modes to the enzyme, the attempt to explain the origin of the inhibitory a...

journal_title：Current medicinal chemistry

authors： Zhang X,Xu W

更新日期：2008-01-01 00:00:00

abstract：:Irinotecan, a camptothecin analogue, is a prodrug which requires bioactivation to form the active metabolite SN-38. SN-38 acts as a DNA topoisomerase I poison. Irinotecan has been widely used in the treatment of metastatic colorectal cancer, small cell lung cancer and several other solid tumors. However, large inter-p...

journal_title：Current medicinal chemistry

authors： Ma MK,McLeod HL

更新日期：2003-01-01 00:00:00

abstract：:Cannabinoids in current use such as nabilone activate both CB1 and CB2 receptors. Selective CB2 activation may provide some of the therapeutic effects of cannabinoids, such as their immuno-modulatory properties, without the psychoactive effects of CB1 activation. Therefore, cannabinoid CB2 receptors represent an attra...

journal_title：Current medicinal chemistry

authors： Ashton JC,Wright JL,McPartland JM,Tyndall JD

更新日期：2008-01-01 00:00:00

abstract：AIMS:Salvianolic acid B (Sal B), one of the most active components of Danshen extracts, has beneficial roles in the prevention and treatment of cardiovascular diseases. However, the precise mechanism by which Sal B exerts its effects on vascular cells is unclear. We aimed to elucidate the effects of Sal B on vascular c...

journal_title：Current medicinal chemistry

authors： Lee HJ,Seo M,Lee EJ

更新日期：2014-01-01 00:00:00

abstract：:Hydroxypyridinones (HPs) are a family of N-heterocyclic metal chelators, which have been an attractive target in the development of a variety of new pharmaceutical drugs, due to their high metal chelating efficacy/specificity and easy derivatization to tune the desired biological properties. In fact, along the last de...

journal_title：Current medicinal chemistry

authors： Chaves S,Piemontese L,Hiremathad A,Santos MA

更新日期：2018-01-01 00:00:00

abstract：:5-Aminoisoquinolin-1-one (5-AIQ) is a water-soluble inhibitor of the poly(ADPribose) polymerases (PARPs), lacking isoform-selectivity. Although of only moderate potency in vitro against PARP-1, it is highly active in many assays in cells and in models in vivo, indicating excellent uptake. Optimisation of the several s...

journal_title：Current medicinal chemistry

authors： Threadgill MD

更新日期：2015-01-01 00:00:00

abstract：:The synthesis and biological evaluation of carbohydrate mimetics has begun to more clearly define the diverse roles of carbohydrates in nature. Often the strategy invoves the design and synthesis of glycosyltransferase and glycosidase inhibitors both as tools to elucidate the mechanism of action of these enzymes and a...

journal_title：Current medicinal chemistry

authors： Elhalabi JM,Rice KG

更新日期：1999-02-01 00:00:00

abstract：:Acyclic nucleoside analogues bearing phosphonomethoxy residues in the side chain (ANP) attract much attention due to a very beneficial combination of biological properties. Intensive work of organic chemists during the last two decades resulted in a large panel of new compounds that were evaluated as potential antivir...

journal_title：Current medicinal chemistry

authors： Khandazhinskaya A,Yasko M,Shirokova E

更新日期：2006-01-01 00:00:00

abstract：:Snakes are fascinating creatures and have been residents of this planet well before ancient humans dwelled the earth. Venomous snakes have been a figure of fear, and cause notable mortality throughout the world. The venom constitutes families of proteins and peptides with various isoforms that make it a cocktail of di...

journal_title：Current medicinal chemistry

authors： Waheed H,Moin SF,Choudhary MI

更新日期：2017-01-01 00:00:00

abstract：:Similarly to a series of chronic diseases, essential arterial hypertension (HTN) may be manifested during childhood as a blood pressure (BP) reading which repeatedly rises above the 95(th) percentile of population-specific standards. Since BP tends to track along the same percentiles throughout life, children with hig...

journal_title：Current medicinal chemistry

authors： Bassareo PP,Bassareo V,Iacovidou N,Mercuro G

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:Smac mimetics (also known as IAP antagonist) are a new class of targeted drugs having a goal to suppress the IAPs, reestablishing the apoptotic pathways and inducing cancer cell death. Therefore, development of Smac mimetics was considered an attractive strategy for the development of new anticancer drugs. L...

journal_title：Current medicinal chemistry

authors： Ali R,Singh S,Haq W

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:The large increase in epidemiological studies on night shift work is due to the important effects of night shift work on workers' health and psychophysical wellbeing. The short-term effects-insomnia, difficulties in managing work and private life, lower work performance, and more work and extra-work accident...

journal_title：Current medicinal chemistry

authors： Ferri GM,Cavone D,Intranuovo G,Macinagrossa L

更新日期：2019-01-01 00:00:00

abstract：:We apply noval techniques, the Scaling Index Method (SIM), which reveals local topology of the structure, and the Minkowski Functionals (MF), which provide four global topological characteristics, to assess strength of the trabecular network of the human bone. We compare capabilities of these methods with the standard...

journal_title：Current medicinal chemistry

authors： Sidorenko I,Monetti R,Bauer J,Mueller D,Rummeny E,Eckstein F,Matsuura M,Lochmueller EM,Zysset P,Raeth C

更新日期：2011-01-01 00:00:00

abstract：:Studies on enzyme inhibition remain an important area of pharmaceutical research since these studies have led to the discoveries of drugs useful in a variety of physiological conditions. The enzyme inhibitors can interact with enzymes and block their activity towards natural substrates. Urease inhibitors have recently...

journal_title：Current medicinal chemistry

authors： Amtul Z,Rahman AU,Siddiqui RA,Choudhary MI

更新日期：2002-07-01 00:00:00

abstract：OBJECTIVE:We found a novel marine drug, SZ-685C, that was isolated from the secondary metabolites of a mangrove endophytic fungus (No. 1403) collected from the South China Sea, which has been reported to inhibit the proliferation of certain tumor cells. However, its anticancer mechanism remains unknown. The aims of thi...

journal_title：Current medicinal chemistry

authors： Chen CH,Xiao WW,Jiang XB,Wang JW,Mao ZG,Lei N,Fan X,Song BB,Liao CX,Wang HJ,She ZG,Zhu YH

更新日期：2013-01-01 00:00:00

abstract：:Cardiovascular pathologies in the French are not prevalent despite high dietary saturated fat consumption. This is commonly referred to as the "French Paradox" attributing its anti-lipidemic effects to moderate consumption of red wine. Resveratrol, a phytoalexin found in red wine, is currently the focus of intense res...

journal_title：Current medicinal chemistry

authors： Raval AP,Lin HW,Dave KR,Defazio RA,Della Morte D,Kim EJ,Perez-Pinzon MA

更新日期：2008-01-01 00:00:00

abstract：:Heterocyclic compounds represent a significant target for anti-cancer research and drug discovery, due to their structural and chemical diversity. Oxazoles, with oxygen and nitrogen atoms present in the core structure, enable various types of interactions with different enzymes and receptors, favoring the discovery of...

journal_title：Current medicinal chemistry

authors： Chiacchio MA,Lanza G,Chiacchio U,Giofrè SV,Romeo R,Iannazzo D,Legnani L

更新日期：2019-01-01 00:00:00

abstract：:The therapeutical use of drugs involves the application of dosage forms, serving as carrier systems together with several excipients to deliver the active ingredient to the site of action. Drug delivery technology combines an understanding of medicinal chemistry and pharmacology with the skill of formulation, aiming t...

journal_title：Current medicinal chemistry

authors： Kalász H,Antal I

更新日期：2006-01-01 00:00:00

abstract：:The development of biodegradable nanoparticles is an important tool for the biological transport of chemical compounds. The nanoencapsulation reduces the biopharmaceutical and pharmacokinetic drawbacks of compounds and enhances their biological properties. Naturally occurring polymers such as proteins and polysacchari...

journal_title：Current medicinal chemistry

authors： Lopes VF,Giongo CN,de Almeida Campos L,Abraham WR,Mainardes RM,Khalil NM

更新日期：2020-11-24 00:00:00

abstract：:Since the discovery of penicillin, natural and synthetic β-lactams have aroused great interest not only as sources of effective antibacterial agents but also as specific inhibitors of proteases responsible for various non-bacterial pathological processes. This interest was reflected in our review published in Current ...

journal_title：Current medicinal chemistry

authors： Veinberg G,Potorocina I,Vorona M

更新日期：2014-01-01 00:00:00

abstract：:Magnetic resonance imaging (MRI) contrast agents are utilized adjunctively to enhance the contrast between normal and abnormal structures on MRI scans. Along with the rapid evolution of the field has come a new appreciation for the medicinal chemistry of this unique class of metallopharmaceuticals. The efficacy of MRI...

journal_title：Current medicinal chemistry

authors： Zhang Z,Nair SA,McMurry TJ

更新日期：2005-01-01 00:00:00

abstract：:The oxime formation reaction of therapeutical progestogen (levonorgestrel, levonorgestrel acetate, norethisterone), androgen (methyltestosterone, testosterone phenylpropionate) and anabolic (nortestosterone phenylpropionate) Delta(4)-3-ketosteroids has been investigated. The ketosteroid-hydroxylamine reaction was moni...

journal_title：Current medicinal chemistry

authors： Szentesi A,Gergely A,Horváth P,Mahó S,Mátyus P,Szász G

更新日期：2001-09-01 00:00:00

abstract：BACKGROUND:Fatty liver, or steatosis, is a condition of excess accumulation of lipids, mainly under form of triglycerides (TG), in the liver, and it is the hallmark of non-alcoholic fatty liver disease (NAFLD). NAFLD is the most common liver disorder world-wide and it has frequently been associated with obesity, hyperl...

journal_title：Current medicinal chemistry

authors： Vergani L

更新日期：2019-01-01 00:00:00

abstract：:Antimitotics binding at the colchicine site of tubulin are important antitumour and vascular disrupting agents. Pyridines and azines are privileged scaffolds in medicinal chemistry and in recent years many colchicine site ligands (CSL) have incorporated them into their structures with the aim of improving their pharma...

journal_title：Current medicinal chemistry

authors： Álvarez R,Aramburu L,Puebla P,Caballero E,González M,Vicente A,Medarde M,Peláez R

更新日期：2016-01-01 00:00:00

abstract：:Currently, the long-term usage of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in HIVAIDS patients eventually leads to the development of drug resistance and severe side effect. Therefore, it is imperative to look for the novel NNRTIs with potent and broad spectrum anti-mutant activity that are also safe a...

journal_title：Current medicinal chemistry

authors： Zhan P,Liu X,Li Z

更新日期：2009-01-01 00:00:00

abstract：:Photodynamic therapy (PDT) involves the administration of a photosensitizer (PS) followed by illumination with visible light, leading to generation of reactive oxygen species. The mechanisms of resistance to PDT ascribed to the PS may be shared with the general mechanisms of drug resistance, and are related to altered...

journal_title：Current medicinal chemistry

authors： Casas A,Di Venosa G,Hasan T,Al Batlle

更新日期：2011-01-01 00:00:00

abstract：:Mycobacterium tuberculosis (Mtb), the main aetiological agent of tuberculosis (TB) in humans, is estimated to cause nearly two million deaths every year. Despite their huge therapeutic value, existing antitubercular drugs have several shortcomings, such as for instance the insurgence of drug resistance, which is mostl...

journal_title：Current medicinal chemistry

authors： Fanzani L,Porta F,Meneghetti F,Villa S,Gelain A,Lucarelli AP,Parisini E

更新日期：2015-01-01 00:00:00

abstract：:Statins are inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate-limiting enzyme of cholesterol synthesis. In recent years, statins have become the major choice of treatment for hypercholesterolemia. Emerging evidence from both animal and human studies indicates that mechanisms i...

journal_title：Current medicinal chemistry

authors： Luo JD,Chen AF

更新日期：2003-08-01 00:00:00

abstract：:A dramatical decline in human male reproductive function has been reported for the past 20 years. Many recent epidemiological, clinical and experimental findings suggest that the reproductive dysfunction could result from prenatal and neonatal chemical compound exposure. Even if numerous studies argue for a relationsh...

journal_title：Current medicinal chemistry

authors： Gilleron J,Malassiné A,Carette D,Segretain D,Pointis G

更新日期：2011-01-01 00:00:00