Cyclin-dependent kinase 7 inhibitors in cancer therapy.

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：:The pharmacokinetic treatment strategy targets the drug molecule itself, aiming to reduce drug concentration at the site of action, thereby minimizing any pharmacodynamic effect. This approach might be useful in the treatment of acute drug toxicity/overdose and in the long-term treatment of addiction. Phase IIa contro...

journal_title：Future medicinal chemistry

authors： Gorelick DA

更新日期：2012-02-01 00:00:00

abstract：BACKGROUND:Since trifluoromethyl-containing compounds have found diverse applications in the fields of pharmaceuticals and agrochemicals, facile and selective synthetic methods for trifluoromethyl-substituted compounds are an essential tool for advanced medicinal chemistry. Now that diverse synthetic transformations of...

journal_title：Future medicinal chemistry

authors： Shimizu M,Higashi M,Takeda Y,Murai M,Jiang G,Asai Y,Nakao Y,Shirakawa E,Hiyama T

更新日期：2009-08-01 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：:In total, 47,500,000 people worldwide are affected by dementia and this number is estimated to double by 2030 and triple within 2050 resulting in a huge burden on public health. Alzheimer's disease (AD), a progressive neurodegenerative disorder, is the most common cause of dementia, accounting for 60-70% of all the ca...

journal_title：Future medicinal chemistry

authors： Stotani S,Giordanetto F,Medda F

更新日期：2016-04-01 00:00:00

abstract：:Aim: Alzheimer's disease (AD) is known to be themajor cause of dementia among the elderly. The structural properties and binding interactions of the AD drug physostigmine (-)-phy, and its analogues (-)-hex and (-)-phe and (+)-phe, were examined, as well as their impact on the conformational changes of two different AD...

journal_title：Future medicinal chemistry

authors： Adeniyi AA,Conradie J

更新日期：2019-08-01 00:00:00

abstract：:Matrix metalloproteinases are zinc-dependent enzymes whose main function is to cleave the components of the extracellular matrix. Their overexpression is evident in all cancers but to date there is no satisfactory way to inhibit their actions. Here, we look at their types, their structures, their functions and the dev...

journal_title：Future medicinal chemistry

authors： King SE

更新日期：2016-01-01 00:00:00

abstract：AIM:Due to the complex nature of Alzheimer's disease, there is a renewed search for pleiotropic agents. RESULTS:Purine+coumarin hybrids have been synthesized and tested for the potential treatment of Alzheimer's disease. Hybrids 6, 4a-b, 14c and 14e inhibit significantly soybean lipoxygenase, whereas derivatives 14b, ...

journal_title：Future medicinal chemistry

authors： Kallitsakis MG,Yañez M,Soriano E,Marco-Contelles J,Hadjipavlou-Litina DJ,Litinas KE

更新日期：2015-01-01 00:00:00

abstract：:Alzheimer's disease is a multifactorial syndrome, for which effective cures are urgently needed. Seeking for enhanced therapeutic efficacy, multitarget drugs have been increasingly sought after over the last decades. They offer the attractive prospect of tackling intricate network effects, but with the benefits of a s...

journal_title：Future medicinal chemistry

authors： Rosini M,Simoni E,Caporaso R,Minarini A

更新日期：2016-04-01 00:00:00

abstract：:Responsive optical probes play a vital role in following and understanding biological events. In this review, we focus on the use of lanthanide complexes as molecular probes, as they offer many advantages in imaging and assays, particularly when used in time-gated protocols. We describe systems that illustrate the key...

journal_title：Future medicinal chemistry

authors： Allain C,Faulkner S

更新日期：2010-03-01 00:00:00

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：BACKGROUND:The objective of this study was to develop and evaluate a more effective mucoadhesive thiomer for buccal drug-delivery systems. METHODS:2-iminothiolane was covalently attached to a chitosan backbone. A preactivation step followed, mediated by 6,6´dithionicotinamide, thiol groups were modified by disulfide b...

journal_title：Future medicinal chemistry

authors： Laffleur F,Shahnaz G,Islambulchilar Z,Bernkop-Schnürch A

更新日期：2013-04-01 00:00:00

abstract：BACKGROUND:Cucurbit[n]urils (CB[n]; n = 5, 6, 7, 8 or 10) are a family of macrocycles made from the acid-catalyzed condensation of glycoluril and formaldehyde. RESULTS:The synthesis of CB[n] using microwave radiation has been examined and the effect of acid type, reaction time and temperature on the distribution of pr...

journal_title：Future medicinal chemistry

authors： Wheate NJ,Patel N,Sutcliffe OB

更新日期：2010-02-01 00:00:00

abstract：AIM:The use of 3D information has shown impact in numerous applications in drug design. However, it is often under-utilized and traditionally limited to specialists. We want to change that, and present an approach making 3D information and molecular modeling accessible and easy-to-use 'for the people'. METHODOLOGY/RES...

journal_title：Future medicinal chemistry

authors： Grebner C,Norrby M,Enström J,Nilsson I,Hogner A,Henriksson J,Westin J,Faramarzi F,Werner P,Boström J

更新日期：2016-09-01 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：:This review provides an overview of chemokines and their receptors, with an emphasis on general features and nomenclature along with a short summary of their properties and functions. It is intended as an introduction to the subject and a reference point for those wishing to learn key facts about chemokines and their ...

journal_title：Future medicinal chemistry

authors： Vinader V,Afarinkia K

更新日期：2012-05-01 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：: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：: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：BACKGROUND:Traditional and current opioid pharmacology is fundamentally based on interactions between opioid receptors and compounds isolated from natural sources. Adverse effects associated with opioids have led to the search for compounds with diminished side effects. DISCUSSION:Recent discoveries of non-nitrogenous...

journal_title：Future medicinal chemistry

authors： Lovell KM,Simpson DS,Cunningham CW,Prisinzano TE

更新日期：2009-05-01 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：:Carbonic anhydrases (CAs; EC 4.2.1.1) are well known zinc metalloproteins involved in the catalysis of a very simple but essential physiological reaction: carbon dioxide hydration to bicarbonate and proton. These enzymes are of clinical relevance in cancer therapy as among the 15 isoforms known in humans, two cell sur...

journal_title：Future medicinal chemistry

authors： Supuran CT,Winum JY

更新日期：2015-01-01 00:00:00

abstract：:Every organism is in contact with numerous small molecules (<1000 Da). Chemicals may cause or trigger adverse health effects, including diseases of the immune system. They may also be exploited as drugs. In this review, we look at the interaction between small molecules and the immune system. We discuss the hapten and...

journal_title：Future medicinal chemistry

authors： Kadow S,Jux B,Chmill S,Esser C

更新日期：2009-12-01 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：BACKGROUND:The pathogenicity of influenza A and B viruses depends on the function of influenza neuraminidase (NA). Emerging resistant influenza A viruses of subtype H1N1 increasingly challenge the effectiveness of established NA inhibitors. Recent computational studies have indicated several weak points of NA that can ...

journal_title：Future medicinal chemistry

authors： Kirchmair J,Rollinger JM,Liedl KR,Seidel N,Krumbholz A,Schmidtke M

更新日期：2011-03-01 00:00:00

abstract：:FGFs and their receptors (FGFRs) are critical for many biologic processes, including angiogenesis, wound healing and tissue regeneration. Aberrations in FGFR signaling are common in cancer, making FGFRs a promising target in antitumor studies. To date, many FGFR inhibitors are being detected in clinical studies, and r...

journal_title：Future medicinal chemistry

authors： Xue WJ,Li MT,Chen L,Sun LP,Li YY

更新日期：2018-09-01 00:00:00

abstract：:Aim: Cysteine proteases are important molecular targets involved in the replication, virulence and survival of parasitic organisms, including Trypanosoma and Leishmania species. Methodology & results: Analogs of the 7-chloro-N-[3-(morpholin-4-yl)propyl]quinolin-4-amine were synthesized and their inhibitory activity ag...

journal_title：Future medicinal chemistry

authors： Andrade MM,Martins LC,Marques GV,Silva CA,Faria G,Caldas S,Dos Santos JS,Leclercq SY,Maltarollo VG,Ferreira RS,Oliveira RB

更新日期：2020-04-01 00:00:00

abstract：:The development of novel pharmaceutical treatments for disorders of the cerebral vasculature is a serious unmet medical need. These vascular disorders are typified by a disruption in the delicate Rho signaling equilibrium within the blood vessel wall. In particular, Rho kinase overactivation in the smooth muscle and e...

journal_title：Future medicinal chemistry

authors： Bond LM,Sellers JR,McKerracher L

更新日期：2015-01-01 00:00:00

abstract：:Aim: To encapsulate amphotericin B (AmB) with reduced toxicity and comparable activity. Results & methodology: The α-linolenic acid (ALA)-modified monomethoxy polyethylene glycol-g-PEI-g-ALA conjugate was employed to prepare AmB-loaded micelles (AmB-M). In vitro activity and release behavior of AmB-M were investigated...

journal_title：Future medicinal chemistry

authors： Xu H,Teng F,Zhou F,Zhu L,Wen Y,Feng R,Song Z

更新日期：2019-10-01 00:00:00

abstract：:The pharmaceutical industry is facing numerous, well-documented challenges - from the effects of patent expirations to high attrition rates in the drug-development pipeline. Future Medicinal Chemistry has invited a group of leaders from academia and industry to express their views on where the industry is heading and ...

journal_title：Future medicinal chemistry

authors： Cottens S,Eaton M,Fuhr J,Geary S,Johnson DS,Li G,Raveglia L,Robertson GM,Westwell A

更新日期：2011-11-01 00:00:00