Microwave-assisted synthesis of bioactive quinazolines and quinazolinones.

abstract：:Survival of cells and maintenance of genome depend on detection and repair of damaged DNA through intricate mechanisms. Cancer treatment relies on chemotherapy or radiation therapy that kills neoplastic cells by causing immense damage to the DNA. In many cases, escalated DNA repair mechanism leads to resistance agains...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jain R,Jamal S,Goyal S,Wahi D,Singh A,Grover A

更新日期：2015-01-01 00:00:00

abstract：:The important factor which differentiates gemini surfactants from conventional monomeric surfactants is the spacer group. The molecular connectivity method was used to study the effect of the spacer group on critical micelle concentration of cationic gemini surfactants. Two models were derived employing only Kier and ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Mozrzymas A

更新日期：2016-01-01 00:00:00

abstract：:This review describes computational procedures for deriving the amino acid sequences that are compatible with a given protein backbone structure. Such procedures can be used to gain insight into the constraints imposed by the 3D structure of the protein sequence, or to design proteins that are likely to adopt a given ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jaramillo A,Wernisch L,Hery S,Wodak SJ

更新日期：2001-12-01 00:00:00

abstract：:Due to the numerous challenges in hit identification from random RNAi screening, we have examined current practices with a discovery of a variety of methodologies employed and published in many reports; majority of them, unfortunately, do not address the minimum associated criteria for hit nomination, as this could po...

journal_title：Combinatorial chemistry & high throughput screening

authors： Bhinder B,Djaballah H

更新日期：2012-11-01 00:00:00

abstract：:The section on patent review will be focused in the areas of interest to the readers of CCHTS. The search was conducted using the following key words: combinatorial chemistry, high throughput screening, drug repurposing, chemical library, high content screening, drug discovery and natural products. All patents highlig...

journal_title：Combinatorial chemistry & high throughput screening

authors： Roy A

更新日期：2011-05-01 00:00:00

abstract：AIM AND OBJECTIVE:Lysine acetylation, as one type of post-translational modifications (PTM), plays key roles in cellular regulations and can be involved in a variety of human diseases. However, it is often high-cost and time-consuming to use traditional experimental approaches to identify the lysine acetylation sites. ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Gao J,Tao XW,Zhao J,Feng YM,Cai YD,Zhang N

更新日期：2017-01-01 00:00:00

abstract：:Increasingly, combinatorial libraries are used to screen large numbers of complex chemically- and physically-patterned polymers against cell response. There is a strong need to extract meaningful relationships between cell function and material surface features from these experiments. A novel high-throughput cell-mate...

journal_title：Combinatorial chemistry & high throughput screening

authors： Su J,Meredith JC

更新日期：2009-07-01 00:00:00

abstract：:A biomimetic sensor is proposed as a promising new analytical method for determination of captopril in different classes of samples. The sensor was prepared by modifying a carbon paste electrode with iron (II) phthalocyanine bis(pyridine) [FePc(dipy)] complex. Amperometric measurements in a batch analytical mode were ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Wong A,Lanza MR,Sotomayor MD

更新日期：2010-09-01 00:00:00

abstract：:In pursuit of utilizing combinatorial peptide libraries on beads, rapid and robust screening is one of the key steps for the success of high-throughput process. We have introduced improved structural features that greatly facilitate a MALDI-MS/MS-based sequencing, associated with easy and fast synthesis and analysis o...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jee JE,Ang YL,Cha J,Ang MW,Ling J,Lim J,Lee SS

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:A set of antibiotic fluoroquinolones with confirmed antimicrobial activity were analyzed with the use of two types of quantum chemical calculation methods and quantitative structure-activity relationships (QSAR). OBJECTIVE:The purpose of this study was to demonstrate the common and differentiating character...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kawczak P,Bober L,Bączek T

更新日期：2018-01-01 00:00:00

abstract：:We have developed a high throughput assay for the measurement of protease activity in solution. This technology will accelerate research in functional proteomics and enable biologists to streamline protease substrate evaluation and optimization. The peptide sequences that serve as protease substrates in this assay are...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kozlov IA,Melnyk PC,Zhao C,Hachmann JP,Shevchenko V,Srinivasan A,Barker DL,Lebl M

更新日期：2006-07-01 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：:Organic reactions performed in the absence of solvent in domestic ovens without appropriate temperature control are generally considered as not reproducible, particularly when different instruments are used. For this reason, reproducibility has historically been one of the major issues associated with Microwave-Assist...

journal_title：Combinatorial chemistry & high throughput screening

authors： Díaz-Ortiz A,de la Hoz A,Alcázar J,Carrillo JR,Herrero MA,Fontana A,Muñoz Jde M,Prieto P,de Cózar A

更新日期：2011-02-01 00:00:00

abstract：OBJECTIVE:A significant proportion of patients with early non-small cell lung cancer (NSCLC) can be cured by surgery. The distant metastasis of tumors is the most common cause of treatment failure. Precisely predicting the likelihood that a patient develops distant metastatic risk will help identify patients who can fu...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zhong J,Chen JM,Chen SL,Yi YF

更新日期：2019-01-01 00:00:00

abstract：:The high level of attrition of drugs in clinical development has led pharmaceutical companies to increase the efficiency of their lead identification and development through techniques such as combinatorial chemistry and high-throughput (HTP) screening. Since the major reasons for clinical drug candidate failure other...

journal_title：Combinatorial chemistry & high throughput screening

authors： Shearer TW,Smith KS,Diaz D,Asher C,Ramirez J

更新日期：2005-02-01 00:00:00

abstract：:A general procedure for the synthesis of a large variety of compounds comprising an alpha, beta,-unsaturated carbonyl functionality was developed. The use of one-pot cascade synthesis with (triphenylphosphora-nylidene)ethenone as a versatile reagent for various formations including heterocycles of different ring sizes...

journal_title：Combinatorial chemistry & high throughput screening

authors： Westmana J,Orrling K

更新日期：2002-11-01 00:00:00

abstract：:Genetic mutations/polymorphisms analyses play a great role in genetic and medical research, and clinical diagnosis. Most conventional methods for genetic assay are based on slab gel electrophoresis that is both labor-intensive and time-consuming. Recently, capillary electrophoresis (CE) has been used for genetic analy...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ren J

更新日期：2000-02-01 00:00:00

abstract：:Shotgun phage display cloning is a useful tool for studying interactions between bacterial and host proteins. Libraries are constructed by cloning randomly fragmented prokaryotic DNA into phage mid-vectors. Theoretically, these libraries will consist of phages that together display all proteins encoded by the bacteria...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jacobsson K,Frykberg L

更新日期：2001-04-01 00:00:00

abstract：:The evaluation of the relationships between the hormones involved in the urogenital tract cancer, including bladder, kidney, prostate, and testis, could prove important from diagnostic point of view. The determination of the steroid hormone profiles may likely provide a biomarker for discrimination of hormone-related ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Konieczna L,Belka M,Baczek T,Ruszkowski M,Struck W,Markuszewski M,Kaliszan R,Markuszewski M

更新日期：2013-07-01 00:00:00

abstract：:The breast cancer resistant protein (BCRP) is an important transporter and its inhibitors play an important role in cancer treatment by improving the oral bioavailability as well as blood brain barrier (BBB) permeability of anticancer drugs. In this work, a computational model was developed to predict the compounds as...

journal_title：Combinatorial chemistry & high throughput screening

authors： Belekar V,Lingineni K,Garg P

更新日期：2015-01-01 00:00:00

abstract：:Mitochondria are the center of metabolism and the critical role of aberrant mitochondrial fission in the onset and progression of a wide range of human diseases such as neurodegenerative disorders, cardiovascular disease, ischemic stroke and diabetes, is slowly becoming recognized. Under physiological conditions, mito...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hanumanthappa P,Rajanikant GK

更新日期：2014-01-01 00:00:00

abstract：:African trypanosomes are the causative agent of sleeping sickness. The therapeutics used to control and treat the disease are very ineffective and thus, the development of improved drugs is urgently needed. Recently, new strategies for the design of novel trypanocidals have been put forward. Among them are techniques ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Adler A,Forster N,Homann M,Göringer HU

更新日期：2008-01-01 00:00:00

abstract：OBJECTIVE:Osteopontin (OPN), a phosphorylated sialoprotein, has been shown to overexpress in a variety of cancers and to contribute tumor progression and metastasis by increasing cell migration and adhesion. In the current study, we aimed to investigate the prognostic and predictive role of OPN in patients with advance...

journal_title：Combinatorial chemistry & high throughput screening

authors： Yazici O,Dogan M,Ozal G,Aktas SH,Demirkazik A,Utkan G,Senler FC,Icli F,Akbulut H

更新日期：2020-09-02 00:00:00

abstract：:In this paper, we introduce two nonconventional ionic liquid compounds which are composed of propane sulfonate functionalized organic cations and heteropolyanions as green solid acid catalysts for the highly efficient and green synthesis of 2,3-disubstitutedquinoxaline derivatives. These ionic liquids are in the solid...

journal_title：Combinatorial chemistry & high throughput screening

authors： Vahdat SM,Baghery S

更新日期：2013-09-01 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：:A method for producing tri- and tetrasubstituted ureas from carbamoyl imidazolium salts is presented. Carbamoyl imidazolium salts are prepared from the reaction of N,N carbonyldiimidazole (CDI) with secondary amines, followed by alkylation with iodomethane. These stable salts can be stored for extended periods and ar...

journal_title：Combinatorial chemistry & high throughput screening

authors： Batey RA,Shen M,Santhakumar V,Yoshina-Ishii C

更新日期：2002-05-01 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：AIM AND OBJECTIVE:Lung cancer is a highly heterogeneous cancer, due to the significant differences in molecular levels, resulting in different clinical manifestations of lung cancer patients there is a big difference. Including disease characterization, drug response, the risk of recurrence, survival, etc. Method:Clin...

journal_title：Combinatorial chemistry & high throughput screening

authors： Guo B,Zheng Q

更新日期：2018-01-01 00:00:00

abstract：:Generation of in vitro cellular assays using fluorescence measurements at heterologously expressed NMDA receptors would speed up the process of ligand characterization and enable high-throughput screening. The major drawback to the development of such assays is the cytotoxicity caused by Ca(2+)-flux into the cell via ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hansen KB,Bräuner-Osborne H,Egebjerg J

更新日期：2008-05-01 00:00:00

abstract：INTRODUCTION:Enzymatic degradation of peptidoglycan, a structural cell wall component of Gram-positive bacteria, has attracted considerable attention being a specific target for many known antibiotics. METHODS:Peptidoglycan hydrolases are involved in bacterial lysis through peptidoglycan degradation. β-N-acetylglucosa...

journal_title：Combinatorial chemistry & high throughput screening

authors： Rathee A,Panwar A,Kumari S,Chhibber S,Kumar A

更新日期：2020-11-03 00:00:00