Recent advances in the solid phase synthesis of drug-like heterocyclic small molecules.

abstract：:Voltage-clamp techniques are typically used to study the plasma membrane proteins, such as ion channels and transporters that control bioelectrical signals. Many of these proteins have been cloned and can now be studied as potential targets for drug development. The two approaches most commonly used for heterologous e...

journal_title：Combinatorial chemistry & high throughput screening

authors： Papke RL,Smith-Maxwell C

更新日期：2009-01-01 00:00:00

abstract：BACKGROUND:Lead (Pb) remains a common contaminant in the environment in many parts of the world. Pb exposure adversely affects many human organs, including the gonads, via oxidant and inflammatory marker propagation in affected tissues. Moringa oleifera leaf extract (MOE) is a rich source of antioxidants reported to ha...

journal_title：Combinatorial chemistry & high throughput screening

authors： Albasher G,Alrajhi R,Alshammry E,Almeer R

更新日期：2020-09-23 00:00:00

abstract：:Trivalent lanthanide ions (Ln(3+)) doped inorganic nanocrystals (NCs) have currently attracted reviving interest and come to the forefront in nanophotonics owing to their potential applications in diverse fields such as luminescent biodetection and bioimaging. As an alternative to conventional biolabels, Ln(3+)-doped ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ju Q,Tu D,Liu Y,Zhu H,Chen X

更新日期：2012-08-01 00:00:00

abstract：BACKGROUND:Neurofibromatosis, also known as Von Recklinghausen disease, is a systemic and progressive genetic disease that primarily affects the skin, eyes, nervous system and bones. The disease can occur in a variety of ways and can vary from individuals. Metabolomic-based research using blood samples has enabled new ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Oz O,Koyuncu I,Gonel A

更新日期：2020-12-04 00:00:00

abstract：:A new, efficient, and solvent-free cyclocondensation reaction of arylmethylidenepyruvic acids with 6- aminouracils is presented that uses a catalytic amount of ZnO nanoparticles (ZnO Nps) as a recyclable catalyst at 70 °C. This protocol has the advantages of high yields (91-98%), easy work-up, very short reaction time...

journal_title：Combinatorial chemistry & high throughput screening

authors： Abdolmohammadi S

更新日期：2013-01-01 00:00:00

abstract：:The Nobel Prize in Chemistry 1902 was given to Hermann Emil Fischer "in recognition of the extraordinary services he had rendered by his work on sugar and purine synthesis". This truly great chemist of all time named a group of bicyclic nitrogenous structures as purines, discovered the synthesis of glucose, fructose a...

journal_title：Combinatorial chemistry & high throughput screening

authors： Franzén R,Tois J

更新日期：2003-08-01 00:00:00

abstract：BACKGROUND:In recent years, Staphylococcus aureus have developed resistance to medicines used for the treatment of human infections. Therefore, the search for antibacterial agents of high potency against Staphylococcus aureus is of great concern. Peptide deformylase (PDF), a metalloprotease catalyzing the removal of a ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Liang L,Zhou Q,Hao Z,Wang F,Zhu Y,Lin Q,Gao J

更新日期：2018-01-01 00:00:00

abstract：:We have developed high throughput fluorescence cell imaging methods to screen chemical libraries for compounds with effects on diverse aspects of cell physiology. We describe screens for compounds that arrest cells in mitosis, that block cell migration, and that block the secretory pathway. Each of these screens yield...

journal_title：Combinatorial chemistry & high throughput screening

authors： Yarrow JC,Feng Y,Perlman ZE,Kirchhausen T,Mitchison TJ

更新日期：2003-06-01 00:00:00

abstract：:4-Benzothiazol-2-ylamino-4-oxo-2-butenoic acid, prepared from reaction of 2-aminobenzothiazole and maleic anhydride, are used as an acid component in Passerini three-component reaction, under solvent-free media, to produce unsaturated α-benzothiazole acyloxyamides in good yields. ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Sheikholeslami-Farahani F,Shahvelayati AS

更新日期：2013-11-01 00:00:00

abstract：AIM AND OBJECTIVE:This study was designed to explore the active compounds and significant pathways of Guizhi-Shaoyao-Zhimu decoction (GSZD) for treating diabetes mellitus using molecular docking combined with network pharmacology. MATERIALS AND METHODS:Chemical constituents of GSZD and diabetes-related target proteins...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zhang Q,Li R,Peng W,Zhang M,Liu J,Wei S,Wang J,Wu C,Gao Y,Pu X

更新日期：2019-01-01 00:00:00

abstract：:The transmembrane metzinkin-proteases of the ADAM (a disintegrin and a metalloproteinase)-family ADAM10 and ADAM 17 are both implicated in the ectodomain shedding of various cell surface molecules including the IL6-receptor and the transmembrane chemokines CX3CL1 and CXCL16. These molecules are constitutively released...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ludwig A,Hundhausen C,Lambert MH,Broadway N,Andrews RC,Bickett DM,Leesnitzer MA,Becherer JD

更新日期：2005-03-01 00:00:00

abstract：:Among the various parasitic diseases, malaria is the deadliest one. Due to the emergence of high drug resistance to the existing drug candidates there is a global need for development of new drug candidates which will be effective against resistant strains of malaria parasite. In silico molecular modeling approaches h...

journal_title：Combinatorial chemistry & high throughput screening

authors： Barmade MA,Murumkar PR,Sharma MK,Shingala KP,Giridhar RR,Yadav MR

更新日期：2015-01-01 00:00:00

abstract：:Direct renin inhibitors (DRIs) have increasingly shown a significant advantage in the treatment of hypertension and protection of target organs. In this paper, a series of azaindole class renin inhibitors were subjected to 3D-QSAR study using Topomer CoMFA. Five kinds of splitting mode for different fragment cutting a...

journal_title：Combinatorial chemistry & high throughput screening

authors： Xiang Y,Song J,Zhang Z

更新日期：2014-01-01 00:00:00

abstract：:Sequential injection analysis (SIA) has been employed as the platform for the development of a high throughput automated assay for glutathione (GSH) in nutrition supplements. The proposed assay is based on the on-line formation of a UV-absorbing thioacrylate derivative (lambda(max) = 285 nm) upon reaction of thiol wit...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zacharis CK,Tzanavaras PD

更新日期：2010-07-01 00:00:00

abstract：:An efficient synthesis of 1,3-oxathiolan-2-yliden derivatives is described via a simple reactions between CHacids, CS2 and oxiranes in the presence of triethylamine at 70° C in water as the solvent. The mild reaction conditions and high yields of the products exhibit the good synthetic advantage of this method. ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Rostami-Charati F,Hosseini-Tabatabaei MR,Shahraki M

更新日期：2014-01-01 00:00:00

abstract：:There is increasing evidence that redox regulation of transcription, particularly activator protein-1 (AP-1) and nuclear factor kappa B (NF-kappaB), is important in inflammatory diseases. Human thioredoxin (TRX), a member of the oxidoreductase superfamily, was initially identified, as a factor which augments the produ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Eguchi M,McMillan M,Nguyen C,Teo JL,Chi EY,Henderson WR Jr,Kahn M

更新日期：2003-11-01 00:00:00

abstract：:A pulsed ultrafiltration-mass spectrometric screening assay has been developed to generate and identify electrophilic metabolites of xenobiotic compounds formed by hepatic cytochrome P450 enzymes. This assay would be suitable for the early identification of potentially toxic compounds during the initial phase of drug ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Nikolic D,Fan PW,Bolton JL,van Breemen RB

更新日期：1999-06-01 00:00:00

abstract：:EGFR (ErbB-1/HER1) kinase plays an important role in cancer therapy. Two classification models were established to predict whether a compound is an inhibitor or a decoy of human EGFR (ErbR-1) by using Kohonen's self-organizing map (SOM) and support vector machine (SVM). A dataset containing 1248 ATP binding site inhib...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kong Y,Qu D,Chen X,Gong YN,Yan A

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:Considering the low ocular bioavailability of conventional formulations used for ocular bacterial infection treatment, there's a need for designing efficient novel drug delivery systems that may enhance of precorneal retention time and corneal permeability. AIM AND OBJECTIVE:The current research focuses on ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kırımlıoğlu GY,Özer S,Büyükköroğlu G,Yazan Y

更新日期：2020-04-27 00:00:00

abstract：:Therapeutic options for many infections are extremely limited and at crisis point. We run the risk of entering a second pre-antibiotic era. There had been no miracle drug for the patients infected by resistant microbial pathogens. Most of the very few new drugs under development have problems with their toxicity, or p...

journal_title：Combinatorial chemistry & high throughput screening

authors： Phougat N,Khatri S,Singh A,Dangi M,Kumar M,Dabur R,Chhillar AK

更新日期：2014-01-01 00:00:00

abstract：:Plasmodium falciparum is the most lethal form of the genus Plasmodium which causes malaria, a 'disease of antiquity'. Globally it affects the health and socio-economic development of a large population especially in Sub-Saharan Africa and Southeast Asia. The Plasmodium falciparum dihydrofolate reductase-thymidylate sy...

journal_title：Combinatorial chemistry & high throughput screening

authors： Borkakoty B,Sarma K,Parida P,Prakash A,Mohapatra PK,Mahanta J

更新日期：2014-01-01 00:00:00

abstract：:Centaurea solstitialis L. ssp. solstitialis (CSS) has been used as medicine for various diseases. In this work, root, stem and flower parts of the plant were separately extracted with methanol to execute bioassay-guided isolation. Antiproliferative activities of each extracts on C6 cells (Rat Brain tumor cells) and He...

journal_title：Combinatorial chemistry & high throughput screening

authors： Erenler R,Sen O,Yaglioglu AS,Demirtas I

更新日期：2016-01-01 00:00:00

abstract：:A comparative structure-affinity study of anthraquinone dyes adsorption on cellulose fibre is presented in this paper. We used receptor-dependent 4D-QSAR methods based on grid and neural (SOM) methodology coupled with IVEPLS procedure. The applied RD 4D-QSAR approach focuses mainly on the ability of mapping dye proper...

journal_title：Combinatorial chemistry & high throughput screening

authors： Bak A,Wyszomirski M,Magdziarz T,Smolinski A,Polanski J

更新日期：2014-01-01 00:00:00

abstract：:The appropriate selection of initial receptor structure has been the 'cornerstone' or foundation of successful structure-based virtual screening (SBVS), and plagued the structure-based design with a significantly practical problem to determine the major physiological states or important transition states of receptors ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zhao Y,Wang H,Zang Y,Zhu X,Zhang S,Zhang L

更新日期：2020-11-10 00:00:00

abstract：:Two approaches were utilized to increase the throughput of pulsed ultrafiltration assays of ligand binding to human serum albumin, reducing the volume of the ultrafiltration chamber and combining pulsed ultrafiltration with high performance liquid chromatography-atmospheric pressure chemical ionization mass spectromet...

journal_title：Combinatorial chemistry & high throughput screening

authors： Gu C,Nikolic D,Lai J,Xu X,van Breemen RB

更新日期：1999-12-01 00:00:00

abstract：:Two tryptophan-modified permethylated beta-cyclodextrins, 6I-L-Trp-6I-deoxy-2I,3I-di-O-methyl-hexakis(2II-VII,3II-VII,6II-VII-tri-O-methyl-beta-cyclodextrin (3) and 6I-D-Trp- 6I-deoxy-2I,3I-di-O-methyl-hexakis(2II-VII,3II-VII,6II-VII-tri-O-methyl)-beta-cyclodextrin (4), were synthesized, and their binding behaviors we...

journal_title：Combinatorial chemistry & high throughput screening

authors： Liu Y,Kang S,Chen Y,Shi J,Ke CF

更新日期：2007-07-01 00:00:00

abstract：:High Throughput experimentation has been well established as a tool in early stage catalyst development and catalyst and process scale-up today. One of the more challenging areas of catalytic research is polymer catalysis. The main difference with most non-polymer catalytic conversions is the fact that the product is ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Gruter GJ,Sipos L,Adrianus Dam M

更新日期：2012-02-01 00:00:00

abstract：:While the in vitro selection of nucleic acid binding species (aptamers) requires numerous liquid-handling steps, these steps are relatively straightforward and the overall process is therefore amenable to automation. Here we demonstrate that automated selection techniques are capable of generating aptamers against a n...

journal_title：Combinatorial chemistry & high throughput screening

authors： Cox JC,Rajendran M,Riedel T,Davidson EA,Sooter LJ,Bayer TS,Schmitz-Brown M,Ellington AD

更新日期：2002-06-01 00:00:00

abstract：:Over the last years microarray technology has become one of the principal platform technologies for the high-throughput analysis of biological systems. Starting with the construction of first DNA microarrays in the 1990s, microarray technology has flourished in the last years and many different new formats have been d...

journal_title：Combinatorial chemistry & high throughput screening

authors： Sobek J,Bartscherer K,Jacob A,Hoheisel JD,Angenendt P

更新日期：2006-06-01 00:00:00

abstract：:P-glycoprotein (P-gp) is well known to cause multidrug resistance (MDR) in cancer cells. This MDR leads to cancer recurrence which is a major obstacle in cancer treatment. High P-gp expression has been observed in the population of cancer stem cells (CSCs) having self-renewal potential. Early detection and inhibition ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Tripathi A,Misra K

更新日期：2016-01-01 00:00:00