Quinoline-based compounds with potential activity against drug-resistant cancers.

abstract：:Variable selection is a procedure used to select the most important features to obtain as much information as possible from a reduced amount of features. The selection stage is crucial. The subsequent design of a quantitative structure-activity relationship (QSAR) model (regression or discriminant) would lead to poor ...

journal_title：Current topics in medicinal chemistry

authors： González MP,Terán C,Saíz-Urra L,Teijeira M

更新日期：2008-01-01 00:00:00

abstract：:Aurora kinases are a group of serine/threonine kinases responsible for the regulation of mitosis. In recent years, with the increase in Aurora kinase-related research, the important role of Aurora kinases in tumorigenesis has been gradually recognized. Aurora kinases have been regarded as a new target for cancer thera...

journal_title：Current topics in medicinal chemistry

authors： Qi G,Liu J,Mi S,Tsunematsu T,Jin S,Shao W,Liu T,Ishimaru N,Tang B,Kudo Y

更新日期：2018-01-01 00:00:00

abstract：:Dipeptidyl peptidase-IV (DPP-IV) (EC 3.4.14.5) is а member of the broad class of hydrolytic enzymes which is responsible for degradation of the incretin peptide hormones regulating blood glucose levels. In this article we review the literature on natural and synthetic DPP-IV inhibitors, focusing their chemical structu...

journal_title：Current topics in medicinal chemistry

authors： Smelcerovic A,Miljkovic F,Kolarevic A,Lazarevic J,Djordjevic A,Kocic G,Anderluh M

更新日期：2015-01-01 00:00:00

abstract：:The problem in this work is the computational characterization of cyclodextrins, crown ethers and hyaluronan (HA) as hosts of inclusion complexes for nanosized drug delivery vehicles in pharmaceutical formulations. The difficulty is addressed through a computational study of some thermodynamic, geometric and topologic...

journal_title：Current topics in medicinal chemistry

authors： Torrens F,Castellano G

更新日期：2015-01-01 00:00:00

abstract：:The field of quantitative structure activity relationships (QSAR) has evolved into an integral tool for pharmaceutical discovery. It is presently an accessible technology, as can be shown by the number papers which are easily found through PubMed literature searches. At one level, QSAR is used routinely and invisibly ...

journal_title：Current topics in medicinal chemistry

authors： Sprous DG,Palmer RK,Swanson JT,Lawless M

更新日期：2010-01-01 00:00:00

abstract：:The dopamine transporter (DAT) is a target for the development of pharmacotherapies for a number of central disorders including Parkinson's disease, Alzheimer's disease, schizophrenia, Tourette's syndrome, Lesch-Nyhan disease, attention deficit hyperactivity disorder (ADHD), obesity, depression, and stimulant abuse as...

journal_title：Current topics in medicinal chemistry

authors： Runyon SP,Carroll FI

更新日期：2006-01-01 00:00:00

abstract：:The chemical versatility of the indole nucleus still inspires the pharmaceutical research to develop innovative suitable indole based drugs. The present work is an overview of the use and application of indole molecule based derivatives, as possible treatment in the main Oxidative Stress related diseases, such as card...

journal_title：Current topics in medicinal chemistry

authors： Aiello F,Valacchi G

更新日期：2014-01-01 00:00:00

abstract：:Autophagy is an important basic metabolic mechanism by engulfing and degrading the unnecessary or dysfunctional cellular components within double-membered autolysosomes to maintain cellular homeostasis. Autophagy has sparkled great interest for its complicated functions in different stages of cancer, and is regarded a...

journal_title：Current topics in medicinal chemistry

authors： Li S,Wang L,Hu Y,Sheng R

更新日期：2015-01-01 00:00:00

abstract：:Melatonin was found to be a potent free radical scavenger in 1993. Since then over 800 publications have directly or indirectly confirmed this observation. Melatonin scavenges a variety of reactive oxygen and nitrogen species including hydroxyl radical, hydrogen peroxide, singlet oxygen, nitric oxide and peroxynitrite...

journal_title：Current topics in medicinal chemistry

authors： Tan DX,Reiter RJ,Manchester LC,Yan MT,El-Sawi M,Sainz RM,Mayo JC,Kohen R,Allegra M,Hardeland R

更新日期：2002-02-01 00:00:00

abstract：:For effective tumour imaging by magnetic resonance imaging (MRI) there is a clear need to develop organ, tissue and cell specific contrast agents that can selectively bind to tumour biomarkers. The versatility of a range of bioconjugation techniques and facile coupling chemistries has facilitated the synthesis of MRI ...

journal_title：Current topics in medicinal chemistry

authors： Kamaly N,Miller AD,Bell JD

更新日期：2010-01-01 00:00:00

abstract：INTRODUCTION:Fabaceae are a rich source of protease inhibitors. METHODS:A proteinaceous protease inhibitor of 25 KDa designated as Macrotyloma uniflorum protease inhibitor (MUPI) was isolated from seeds of Macrotyloma uniflorum and purified to homogeneity by ammonium sulphate precipitation, DEAE Sepharose column and C...

journal_title：Current topics in medicinal chemistry

authors： Mohan M,Elyas KK

更新日期：2018-01-01 00:00:00

abstract：:Natural quinoline alkaloid camptothecin (CPT) is used for the treatment of colon, lung, breast and ovarian cancers still facing challenges due to low solubility in aqueous and biological fluids. Its lactone form easily converts into a toxic carboxylic form at slightly basic pH, typical in blood and tissue fluid has ra...

journal_title：Current topics in medicinal chemistry

authors： Mishra D,Yadav V,Khare P,Jyotshna,Das MR,Meena A,Shanker K

更新日期：2016-01-01 00:00:00

abstract：:The adenosine A(2A) receptor is a member of the G protein-coupled receptor family and mediates multiple physiological effects of adenosine, both at the central nervous system and at peripheral tissues. Increasing evidence relates the A(2A) receptor with several pathological conditions such as neurodegenerative disorde...

journal_title：Current topics in medicinal chemistry

authors： Clementina M,Giuseppe S

更新日期：2010-01-01 00:00:00

abstract：:The introduction of biochemical biomarkers in the evaluation of patients with cardiovascular disease has led to practice-changing advancements in the way these patients are diagnosed and managed. Measurements of cardiac troponins or brain-type natriuretic peptide (BNP) and its precursor, N-terminal brain-type natriure...

journal_title：Current topics in medicinal chemistry

authors： Giannopoulos G,Deftereos S,Panagopoulou V,Kossyvakis C,Kaoukis A,Bouras G,Pyrgakis V,Cleman MW

更新日期：2013-01-01 00:00:00

abstract：:This is a general review of currently available antimalarial drugs, these compounds are gathered according with its chemical structure and the biological targets. A great number of these new antimalarial agents are now moving actively in the pipeline from basic science to clinical studies. ...

journal_title：Current topics in medicinal chemistry

authors： Domínguez JN

更新日期：2002-11-01 00:00:00

abstract：:Machine learning (ML) computational methods for predicting compounds with pharmacological activity, specific pharmacodynamic and ADMET (absorption, distribution, metabolism, excretion and toxicity) properties are being increasingly applied in drug discovery and evaluation. Recently, machine learning techniques such as...

journal_title：Current topics in medicinal chemistry

authors： Dobchev DA,Pillai GG,Karelson M

更新日期：2014-01-01 00:00:00

abstract：:KRAS is the most common oncogene to be mutated in lung cancer, and therapeutics directly targeting KRAS have proven to be challenging. The mutations of KRAS are associated with poor prognosis, and resistance to both adjuvant therapy and targeted EGFR TKI. EGFR TKIs provide significant clinical benefit for patients who...

journal_title：Current topics in medicinal chemistry

authors： He H,Xu C,Cheng Z,Qian X,Zheng L

更新日期：2019-01-01 00:00:00

abstract：:Antimicrobial peptides (AMPs) establish the first line of host defense mechanism against invading microorganisms including bacteria, viruses, fungi and parasites. In recent years, emergence and spread of antibiotic resistance bacterial pathogens have dawn considerable interest in investigations of AMPs. The ability of...

journal_title：Current topics in medicinal chemistry

authors： Bhattacharjya S

更新日期：2016-01-01 00:00:00

abstract：:Glucuronidation has been recognized as an important clearance mechanism in humans. Therefore, knowledge about the contribution of glucuronidation to clearance of drug candidates is of great value in early drug development. In this article, we discuss the recent progress made to predict in vivo glucuronidation paramete...

journal_title：Current topics in medicinal chemistry

authors： Wu B,Dong D,Hu M,Zhang S

更新日期：2013-01-01 00:00:00

abstract：:The low affinity A(2B) adenosine receptor, like any other adenosine receptor subtype, belongs to the super-family of seven transmembrane domain protein-coupled receptors (7TMs GPCR) and is classified by the GPCR database in the family of rhodopsin like receptors (Class A of GPCR). It has been cloned from various speci...

journal_title：Current topics in medicinal chemistry

authors： Volpini R,Costanzi S,Vittori S,Cristalli G,Klotz KN

更新日期：2003-01-01 00:00:00

abstract：BACKGROUND:Biofilm is a critical virulence factor associated with the strains of Candida spp. pathogens as it confers significant resistance to the pathogen against antifungal drugs. METHODS:A systematic review of the literature was undertaken by focusing on natural products, which have been reported to inhibit biofil...

journal_title：Current topics in medicinal chemistry

authors： Singla RK,Dubey AK

更新日期：2019-01-01 00:00:00

abstract：:The scaffold protein Axin plays important roles in multiple signaling pathways through mediating the formation of different signaling complexes. Axin is best known for its role as a negative regulator in Wnt/β-catenin pathway. Aberrant activation of the key components in Wnt/β-catenin pathway including Axin has been l...

journal_title：Current topics in medicinal chemistry

authors： Song X,Cai W,Li L

更新日期：2016-01-01 00:00:00

abstract：:The design of syringeable cyclodextrin (CD) gels is a developing area in the drug delivery and tissue engineering fields, since they offer the possibility of being administered with minimally invasive maneuvers to form depots that can remain for prolonged time in the implantation site. Two different supramolecular sys...

journal_title：Current topics in medicinal chemistry

authors： Simões SM,Veiga F,Torres-Labandeira JJ,Ribeiro AC,Concheiro A,Alvarez-Lorenzo C

更新日期：2014-01-01 00:00:00

abstract：:Much attention has focused on the development of protein kinases as drug targets to treat a variety of human diseases including diabetes, cancer, hypertension and arthritis. To date, Gleevec is one example of a drug targeting protein that has successfully treated human cancer. Several other protein kinase inhibitors a...

journal_title：Current topics in medicinal chemistry

authors： Haystead TA

更新日期：2006-01-01 00:00:00

abstract：:In last decades, diet and dietary components have been regarded as important strategies to prevent the development or mitigate numerous chronic diseases, including inflammation, cardiovascular pathologies, cancer, etc. One of the most common dietary components of Asian population is soy. A plethora of research shows t...

journal_title：Current topics in medicinal chemistry

authors： Nabavi SF,Daglia M,Tundis R,Loizzo MR,Sobarzo-Sanchez E,Orhan IE,Nabavi SM

更新日期：2015-01-01 00:00:00

abstract：:Antimicrobial peptides (AMPs) are a class of peptides found across a wide array of organisms that play key roles in host defense. AMPs induce selective death in target cells and orchestrate specific or nonspecific immune responses. Many AMPs exhibit native anticancer activity in addition to antibacterial activity, and...

journal_title：Current topics in medicinal chemistry

authors： Rubin SJS,Qvit N

更新日期：2020-01-01 00:00:00

abstract：:Alzheimer's disease (AD) is a multifactorial complex disease. The pathogenesis of AD is very complicated, and involves the β-amyloid (Aβ) cascade, tau hyperphosphorylation, neuroinflammation, oxidative stress, mitochondrial dysfunction, reduced levels of neurotrophic factors, and damage and loss of synapses as well as...

journal_title：Current topics in medicinal chemistry

authors： Li L,Zhang L,Yang CC

更新日期：2016-01-01 00:00:00

abstract：:Viral entry, the first process in the reproduction of viruses, primarily involves attachment of the viral envelope proteins to membranes of the host cell. The crucial components that play an important role in viral entry include viral surface glycoprotein gp120, viral transmembrane glycoprotein gp41, host cell glycopr...

journal_title：Current topics in medicinal chemistry

authors： Suttisintong K,Kaewchangwat N,Thanayupong E,Nerungsi C,Srikun O,Pungpo P

更新日期：2019-01-01 00:00:00

abstract：:Ischemic heart disease and cerebrovascular disease are the leading causes of death in the world. Surprisingly, these diseases are treated by relatively antiquated drugs. However, due to our improved understanding of the underlying pathology of these diseases, and a number of technological advances in tools for drug di...

journal_title：Current topics in medicinal chemistry

authors： Leadley RJ Jr

更新日期：2001-06-01 00:00:00

abstract：:Over activation of the NMDA receptor complex has been implicated in a number of neurological conditions. The use of NMDA antagonists as therapeutic agents has been limited by serious cognitive and motor side effects. Significant efforts have been reported in the development of NR2B subtype-selective antagonists, which...

journal_title：Current topics in medicinal chemistry

authors： Layton ME,Kelly MJ 3rd,Rodzinak KJ

更新日期：2006-01-01 00:00:00