Aurora Kinase Inhibitors in Head and Neck Cancer.

abstract：:(2R,3R)-2,3-Butanediol has many industrial applications, such as it is used as an antifreeze agent and low freezing point fuel. In addition, it is particularly important to provide chiral groups in drugs. In recent years, this valuable bio-based chemical has attracted increasing attention, and significant progress has...

journal_title：Current topics in medicinal chemistry

authors： Xie NZ,Chen XR,Wang QY,Chen D,Du QS,Zhou GP,Huang RB

更新日期：2017-01-01 00:00:00

abstract：:Artemisinin is isolated from Artemisia annua L. with peroxide-containing sesquiterpene lactone structure. Because of its unique structural characteristics and promising anticancer, antivirus activities, it has recently received increasing attention. The aim of this review is to summarize recent discoveries of artemisi...

journal_title：Current topics in medicinal chemistry

authors： Liu X,Cao J,Huang G,Zhao Q,Shen J

更新日期：2019-01-01 00:00:00

abstract：:Imidazo[1,2-a]pyridine has been shown to be an important biologically active moiety. This review is a compilation of the scattered output of results of the anticancer activities of the imidazo[1,2-a]pyridine system since 2001, which have been classified as inhibition of CDK, VEGFR, PI3K, EGFR, RGGT etc. along with inh...

journal_title：Current topics in medicinal chemistry

authors： Goel R,Luxami V,Paul K

更新日期：2016-01-01 00:00:00

abstract：:The discovery of small molecule melanin concentrating hormone receptor (MHCr1) antagonists as novel therapeutic agents has been widely pursued across the pharmaceutical industry. While multiple chemotypes of small molecule MCHr1 antagonists have been identified and shown to induce weight loss in rodent models of obesi...

journal_title：Current topics in medicinal chemistry

authors： Judd AS,Souers AJ,Kym PR

更新日期：2008-01-01 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：:Several strategies used in the rational design and synthesis of fluorinated compounds as potential therapeutic agents are reviewed. Applications of fluorine substitution in empirical SAR studies for lead development also are discussed, along with the implications with respect to fluorine target interactions that can b...

journal_title：Current topics in medicinal chemistry

authors： Kirk KL

更新日期：2006-01-01 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 development of computational tools for the prediction of passive transport is reviewed with particular reference to four diverse approaches: the rule-of-5, polar surface area, Volsurf and Abraham's General Solvation Equation. To illustrate the current state of the art, several examples of the application of in sil...

journal_title：Current topics in medicinal chemistry

authors： Clark DE,Grootenhuis PD

更新日期：2003-01-01 00:00:00

abstract：:HIV-1 integrase (IN) plays an important role in the life cycle of HIV and is responsible for integration of the virus into the human genome. We present computational approaches used to design novel HIV-1 IN inhibitors. We created an IN inhibitor database by collecting experimental data from the literature. We develope...

journal_title：Current topics in medicinal chemistry

authors： Guasch L,Zakharov AV,Tarasova OA,Poroikov VV,Liao C,Nicklaus MC

更新日期：2016-01-01 00:00:00

abstract：:Cathepsin S has been of increasing interest as a target of medicinal chemistry efforts given its role in modulating antigen-presentation by major histocompatibility class II (MHC II) molecules as well as its involvement in extracellular proteolytic activities. Inhibition of the cathepsin S enzyme reduces degradation o...

journal_title：Current topics in medicinal chemistry

authors： Wiener JJ,Sun S,Thurmond RL

更新日期：2010-01-01 00:00:00

abstract：:Seizures are one of the most common neurological disorders in clinical medicine. Triggering mechanisms by which seizures form remain unclear, but are related to a rapid change in ionic composition, including an increase of intracellular potassium concentration and pH shifts within the brain. pH buffering of extra- and...

journal_title：Current topics in medicinal chemistry

authors： Thiry A,Dogné JM,Supuran CT,Masereel B

更新日期：2007-01-01 00:00:00

abstract：:Rheumatoid Arthritis (RA) is a chronic autoimmune inflammatory disease that affects largely synovial joints. It has been postulated that activated autoreactive CD4 T cells play a key role in triggering and/or maintaining the chronic inflammatory process in RA. Dendritic cells (DCs) are antigen-presenting cells that ac...

journal_title：Current topics in medicinal chemistry

authors： Rodríguez-Fernández JL

更新日期：2013-01-01 00:00:00

abstract：:Apoptosis is a vital physiological process, which is observed in various biological events. The anti-apoptotic and pro-apoptotic members of Bcl-2 family are the most characterized proteins which are involved in the regulation of apoptotic cell death. The anti-apoptotic proteins such as Bcl-2 and Bcl-xL prevent apoptos...

journal_title：Current topics in medicinal chemistry

authors： Salam AAA,Nayek U,Sunil D

更新日期：2018-01-01 00:00:00

abstract：:In recent years, relationship between free radicals and oxidative stress with aging, cancer, atherosclerosis, neurodegenerative disorders, diabetes, and inflammatory diseases became increasingly clear. Confirming the role of oxidants in numerous pathological conditions such as cancer, the antioxidants developed as the...

journal_title：Current topics in medicinal chemistry

authors： Karaaslan C,Suzen S

更新日期：2015-01-01 00:00:00

abstract：:Cancer is a multifactorial disease including interactions of complex genetic and environmental factors. Clinical efficacy of anticancer chemotherapies is hampered by various factors including multidrug resistance (MDR). There is a strong need to discover more potent novel cancer drugs to kill cancer cells selectively....

journal_title：Current topics in medicinal chemistry

authors： Kucuksayan E,Ozben T

更新日期：2017-01-01 00:00:00

abstract：INTRODUCTION:Mosquito borne diseases continue to propagate and cause millions of deaths annually. They are caused either by protozoan parasites such as Plasmodium, Toxoplasma or by flaviviruses including Dengue and Zika. Among the proteome of such parasitic organisms, proteases play essential roles in events such as ho...

journal_title：Current topics in medicinal chemistry

authors： Pant A,Pasupureddy R,Pande V,Seshadri S,Dixit R,Pandey KC

更新日期：2017-01-01 00:00:00

abstract：:Cells rely on several transition metals to regulate a wide range of metabolic and signaling functions. The diversity and efficiency of their physiological functions are derived from atomic properties that are specific to transition metals, most notably an incomplete inner valence subshell. These properties impart upon...

journal_title：Current topics in medicinal chemistry

authors： Hamai D,Bondy SC,Becaria A,Campbell A

更新日期：2001-12-01 00:00:00

abstract：:This review describes the role of nuclear receptors in the regulation of genes involved in cholesterol transport and synthetic modulators of these receptors. Increasing the efflux of cholesterol from peripheral cells, such as lipid-laden macrophages, through a process called reverse cholesterol transport (RCT) require...

journal_title：Current topics in medicinal chemistry

authors： Pelton PD,Patel M,Demarest KT

更新日期：2005-01-01 00:00:00

abstract：BACKGROUND:Glycogen synthase kinase-3 (GSK-3) is involved in the phosphorylation and inactivation of glycogen synthase. GSK-3 inhibitors have been associated with a variety of diseases, including Alzheimer´s disease (AD), diabetes type II, neurologic disorders, and cancer. The inhibition of GSK-3β isoforms is likely to...

journal_title：Current topics in medicinal chemistry

authors： Francisco CS,Javarini CL,de S Barcelos I,Morais PAB,de Paula H,de S Borges W,Neto ÁC,Lacerda V

更新日期：2020-01-01 00:00:00

abstract：:Of the tropical diseases, trypanosomiases and leishmaniases should most concern the pharmaceutical community because of their high prevalence in developing countries and the lack of effective drug treatments. Despite this, they have not historically received much attention in terms of investment and research effort, n...

journal_title：Current topics in medicinal chemistry

authors： Bolognesi ML

更新日期：2011-11-01 00:00:00

abstract：:R115777 (R)-6-amino[(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone is a potent and selective inhibitor of farnesyl protein transferase with significant antitumor effects in vivo subsequent to oral administration in mice. Taking its roots into Janssen's ketoconazole and...

journal_title：Current topics in medicinal chemistry

authors： Venet M,End D,Angibaud P

更新日期：2003-01-01 00:00:00

abstract：:Pronucleotides represent a promising alternative to improve the biological activity of nucleoside analogues against different viral diseases. The basic idea is to achieve nucleotide delivery into cells, bypassing limitations with intracellular formation of nucleotides from their nucleoside precursors. The cycloSal-con...

journal_title：Current topics in medicinal chemistry

authors： Meiera C,Renzea J,Ducho C,Balzarini J

更新日期：2002-10-01 00:00:00

abstract：:Bacterial infections constitute an always growing health problem worldwide. The resistance to antibiotics of an increasing number of bacterial pathogens necessitates a permanent search for new molecules with different mechanisms of action. Histidine biosynthesis is an ancient pathway found in bacteria, archaebacteria,...

journal_title：Current topics in medicinal chemistry

authors： Monti SM,De Simone G,D'Ambrosio K

更新日期：2016-01-01 00:00:00

abstract：:With the global aging population, Alzheimer's disease, Parkinson's disease and mild cognition impairment are increasing in prevalence. The success of rapamycin as an agent to extend lifespan in various organisms, including mice, brings hope that chronic mTOR inhibition could also refrain age-related neurodegeneration....

journal_title：Current topics in medicinal chemistry

authors： Jahrling JB,Laberge RM

更新日期：2015-01-01 00:00:00

abstract：:Neural activity utilizes energy resources and requires replenishment of metabolites through vascular dilation. During wake, cortical neurons usually have depolarized membrane potentials and exhibit frequent spontaneous action potentials, requiring an increased metabolic delivery to activated tissue and causing blood v...

journal_title：Current topics in medicinal chemistry

authors： Schei JL,Rector DM

更新日期：2011-01-01 00:00:00

abstract：:Rhodiola as one of traditional medicines has been used for clinical treatments due to its strong antioxidant properties. Phytochemical analysis revealed the presence of flavonoids, phenylpropanoids, phenylethanol/benzyl alcohol derivatives, cyanogenic glycosides and terpenoids. The bioactive compounds had been demonst...

journal_title：Current topics in medicinal chemistry

authors： Li Y,Wu J,Shi R,Li N,Xu Z,Sun M

更新日期：2017-01-01 00:00:00

abstract：:Sialorrhea or excessive drooling is a significant medical issue in Parkinson's disease (PD) and neurodegenerative disorders, although it is often underreported by patients. Sialorrhea affects a large proportion of PD patients, ranging up to 78% in advanced stages, with many PD patients considering drooling as their wo...

journal_title：Current topics in medicinal chemistry

authors： Farber NM,Perez-Lloret S,Gamzu ER

更新日期：2015-01-01 00:00:00

abstract：: ...

journal_title：Current topics in medicinal chemistry

authors： Dea-Ayuela MA,Serrano DR

更新日期：2018-01-01 00:00:00

abstract：:The Human Genome Project and the explosion of high-throughput data have transformed the areas of molecular and personalized medicine, which are producing a wide range of studies and experimental results and providing new insights for developing medical applications. Research in many interdisciplinary fields is resulti...

journal_title：Current topics in medicinal chemistry

authors： de la Iglesia D,García-Remesal M,de la Calle G,Kulikowski C,Sanz F,Maojo V

更新日期：2013-01-01 00:00:00

abstract：:Screening and identifying a disease-specific novel drug target is the first step towards a rational drug designing approach. Due to the advent of high throughput data generation techniques, the protein search space has now exceeded 24,500 human protein coding genes, which encodes approximately 1804proteins. This work ...

journal_title：Current topics in medicinal chemistry

authors： Jain B,Raj U,Varadwaj PK

更新日期：2018-01-01 00:00:00