Artificial hematopoietic stem cell niche: bioscaffolds to microfluidics to mathematical simulations.

abstract：:Low drug productivity has been a significant problem of the pharmaceutical industry for several decades even though numerous novel technologies were introduced during this period. Currently pharmacologic dogma, "single drug, single target, single disease", is at the root of the lack of drug productivity. From a system...

journal_title：Current topics in medicinal chemistry

authors： Ye H,Wei J,Tang K,Feuers R,Hong H

更新日期：2016-01-01 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：: ...

journal_title：Current topics in medicinal chemistry

authors： Yu Y

更新日期：2019-01-01 00:00:00

abstract：:Thiosemicarbazones (TSCNs) constitute a broad family of compounds (R1R2C=N-NH-C(S)- NR3R4), particularly attractive because many of them display some biological activity against a wide range of microorganisms and cancer cells. Their activity can be related to their electronic and structural properties, which offer a r...

journal_title：Current topics in medicinal chemistry

authors： Matesanz AI,Herrero JM,Quiroga AG

更新日期：2021-01-01 00:00:00

abstract：:Plasmodium has a complex life cycle that spans between mosquito and human. For survival and pathogenesis it banks upon dynamic alterations in ionic transport across organelle and plasma membrane. Being a fundamental contributor of crucial biological processes in parasite, ionic balance facilitates parasite invasion, a...

journal_title：Current topics in medicinal chemistry

authors： Bharti H,Singal A,Raza M,Ghosh PC,Nag A

更新日期：2019-01-01 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：: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：:Cardiovascular disease represents an unparalleled proportion of the global burden of disease and will remain the main cause of mortality for the near future. Fortunately, most premature cardiovascular deaths are preventable. Therefore, prevention becomes vital and diet has shown beneficial effects to protect from CVD ...

journal_title：Current topics in medicinal chemistry

authors： Núñez-Córdoba JM,Martínez-González MA

更新日期：2011-01-01 00:00:00

abstract：:(18)F-labeled amino acids are an important class of imaging agents for positron emission tomography (PET) that target the increased rates of amino acid transport by many tumor cells. This class of tracers is structurally diverse, and the biological and imaging properties of a given (18)F-labeled amino acid depends lar...

journal_title：Current topics in medicinal chemistry

authors： Huang C,McConathy J

更新日期：2013-01-01 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：:Cardiac fibrosis is associated with most cardiac diseases. Fibrosis is an accumulation of excessive extracellular matrix proteins (ECM) synthesized by cardiac fibroblasts and myofibroblasts. Fibroblasts are the most prevalent cell type in the heart, comprising 75% of cardiac cells. Myofibroblasts are hardly present in...

journal_title：Current topics in medicinal chemistry

authors： Yue Z,Zhang Y,Xie J,Jiang J,Yue L

更新日期：2013-01-01 00:00:00

abstract：:Malaria, caused by protozoa of the genus Plasmodium, remains one of the most dreadful infectious diseases worldwide killing more than 1 million people per year. The emergence of multidrug-resistant parasites highly demands a steadfast and continuous search not only for new targets but also for new anti-infectives addr...

journal_title：Current topics in medicinal chemistry

authors： Wegscheid-Gerlach C,Gerber HD,Diederich WE

更新日期：2010-01-01 00:00:00

abstract：:Hepatitis C virus (HCV) is a major cause of acute hepatitis and chronic liver disease, including cirrhosis and hepatocellular carcinoma (HCC). No vaccine is currently available to prevent hepatitis C, and the current standard of care (SOC) - pegylated interferon-α (PEG-IFN-α) in combination with ribavirin (RBV) - is o...

journal_title：Current topics in medicinal chemistry

authors： Avolio S,Summa V

更新日期：2010-01-01 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：:Integrating physicochemical, drug metabolism, pharmacokinetics, ADME, and toxicity assays into drug discovery in order to reduce the attrition rates in clinical development is reviewed. The review is organized around three main decision points used in discovery including hit generation, lead optimization and final can...

journal_title：Current topics in medicinal chemistry

authors： Caldwell GW,Yan Z,Tang W,Dasgupta M,Hasting B

更新日期：2009-01-01 00:00:00

abstract：:Sporotrichosis is a serious public health problem in Brazil that affects human patients and domestic animals, mainly cats. Thus, the search for new antifungal agents is required also due to the emergence and to the lack of effective drugs available in the therapeutic arsenal. The aim of this study was to evaluate the ...

journal_title：Current topics in medicinal chemistry

authors： da S M Forezi L,Borba-Santos LP,Cardoso MFC,Ferreira VF,Rozental S,de C da Silva F

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:Polyphenols are organic compounds widely found in plants and possess many diverse biological activities. In the current study, eleven polyphenolic compounds [rutin (1), trans-ferulic acid (2), epigallaocatechin gallate (3), fumaric acid (4), chlorogenic acid (5), gallic acid (6), trans-resveratrol (7), propy...

journal_title：Current topics in medicinal chemistry

authors： Rauf A,Orhan IE,Ertas A,Temel H,Hadda TB,Saleem M,Raza M,Khan H

更新日期：2017-01-01 00:00:00

abstract：:Release of somatostatin into the circulation from the activated TRPV1-expressing nociceptors revealed by antidromic stimulation of dorsal roots in the rat pinpointed to a novel potential drug target on these nociceptors. The review summarizes the functional, biochemical and pharmacological evidence for a novel somatos...

journal_title：Current topics in medicinal chemistry

authors： Szolcsányi J,Pintér E,Helyes Z,Petho G

更新日期：2011-01-01 00:00:00

abstract：:In the last few years, there has been a great increase in our understanding of pain mechanisms. Given the complexity of the mechanisms involved in pain modulation, it is surprising that the pharmacological control of pain through the application of relatively simple analgesics can be effective. Nevertheless, the appli...

journal_title：Current topics in medicinal chemistry

authors： Mico JA,Berrocoso E,Ortega-Alvaro A,Gibert-Rahola J,Rojas-Corrales MO

更新日期：2006-01-01 00:00:00

abstract：:Thermolysin (TLN) and other thermolysin-like zinc metalloproteinases (TLPs),are important virulence factors for pathogenesis of bacterial infections by suppressing the innate immune system of the host. Therapeutic inhibition ofTLPs is believed to be a novel strategy inthe development of a new generation antibiotics.In...

journal_title：Current topics in medicinal chemistry

authors： Khan MT,Dedachi K,Matsui T,Kurita N,Borgatti M,Gambari R,Sylte I

更新日期：2012-01-01 00:00:00

abstract：:In this paper we applied the "macromolecular docking" procedure to perform molecular modeling with the aim of screening transcription factor sequences for possible interaction to the HIV-1 TAR-RNA, employing the software Hex version 4.2. The molecular modeling data were compared with electrophoretic mobility shift ass...

journal_title：Current topics in medicinal chemistry

authors： Khan MT,Mischiati C,Ather A,Ohyama T,Dedachi K,Borgatti M,Kurita N,Gambari R

更新日期：2012-01-01 00:00:00

abstract：AIMS:The need to find new antimicrobial agents to cope with this phenomenon increases. BACKGROUND:Infection diseases are illness caused by different microorganisms, such as bacteria, among those caused by resistant bacteria are associated with greater morbidity, mortality and cost of the treatment than those caused by...

journal_title：Current topics in medicinal chemistry

authors： Nocedo-Mena D,Garza-González E,González-Ferrara M,Del Rayo Camacho-Corona M

更新日期：2020-01-01 00:00:00

abstract：:As the first stable tachysterol analogs, 14-epi-19-nortachysterol and its 2-substituted derivatives were synthesized using the Stille coupling reaction between the A-ring precursor (three vinylstannanes) and the CD-ring vinyl trifrate. Among them, the 2-methylidene group was hydrogenated with Wilkinson's catalyst regi...

journal_title：Current topics in medicinal chemistry

authors： Sawada D,Kittaka A

更新日期：2014-01-01 00:00:00

abstract：:This review highlights the biological importance of many polysubstituted nitro-prolines and -pyrrolidines. Their preparation using asymmetric 1,3-dipolar cycloadditions of azomethine ylides with nitroalkenes using diastereoselective and enantioselective strategies is described remarking the scope and main features of ...

journal_title：Current topics in medicinal chemistry

authors： Nejera C,Sansano JM

更新日期：2014-01-01 00:00:00

abstract：:A series of novel derivatives of 1,3-oxazolidin-2-one 12a-12n has been synthesized starting from 4-nitro-(L)- phenylalanine by involving five-step reaction sequence. All the compounds were screened for their in vitro antibacterial activity against four pathogenic bacterial strains namely, Staphylococcus aureus, Bacill...

journal_title：Current topics in medicinal chemistry

authors： Chandna N,Kapoor JK,Goyal V,Aggarwal NK,Kumari KM,Vijjulatha M

更新日期：2013-08-01 00:00:00

abstract：:Cytochrome P450 17A1 (CYP17A1; also P450c17and P450sccII) is a critically important enzyme in humans that catalyzes the formation of all endogenous androgens. It is an atypical cytochrome P450 enzyme in that it catalyzes two distinct types of substrate oxidation. Through its hydroxylase activity, it catalyzes the 17α-...

journal_title：Current topics in medicinal chemistry

authors： Porubek D

更新日期：2013-01-01 00:00:00

abstract：:Prion diseases or transmissible spongiform encephalopathies (TSEs) are fatal neurodegenerative disorders associated with the conformational conversion of the cellular prion protein, PrP(C), into a pathological form known as prion or PrP(Sc). They can be classified into sporadic, inherited and infectious forms. Spontan...

journal_title：Current topics in medicinal chemistry

authors： Biljan I,Ilc G,Giachin G,Legname G,Plavec J

更新日期：2013-01-01 00:00:00

abstract：:Non-selective NSAIDs enhance the risk of serious ulcer complications (bleeding, perforation, obstruction), hospitalization and death about 3-10-fold. The gastrointestinal side effects of NSAIDs have a considerable economical burden, since they are responsible for 5-10 billion dollars in hospitalization charges and los...

journal_title：Current topics in medicinal chemistry

authors： Lehmann FS,Beglinger C

更新日期：2005-01-01 00:00:00

abstract：:Several non-cardiovascular drugs have been withdrawn from the market due to their inhibition of hERG K+ channels that can potentially lead to severe heart arrhythmia and death. As hERG safety testing is a mandatory FDArequired procedure, there is a considerable interest for developing predictive computational tools to...

journal_title：Current topics in medicinal chemistry

authors： Braga RC,Alves VM,Silva MF,Muratov E,Fourches D,Tropsha A,Andrade CH

更新日期：2014-01-01 00:00:00

abstract：:Autoimmune diseases are characterized by the production of autoantibodies directed against specific organs of own organism. Additional common traits of autoimmune diseases are chronic inflammation due to generation of inflammatory mediators, and disorders of redox processes. The pathogenesis of autoimmune diseases is ...

journal_title：Current topics in medicinal chemistry

authors： Tomczynska M,Bijak M,Saluk J

更新日期：2016-01-01 00:00:00