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A family of carbonyl-substituted diphenylpyrimidine derivatives (Car-DPPYs) with strong activity against focal adhesion kinase (FAK), were described in this manuscript. Among them, compounds 7a (IC = 5.17 nM) and 7f (IC = 2.58 nM) displayed equal anti-FAK enzymatic activity to the lead compound TAE226 (6.79 nM). In particular, compound 7a also exhibited strong antiproliferative activity against several stubborn cancer cells, including AsPC-1 cells (IC = 0.105 μM), BxPC-3 cells (IC = 0.090 μM), and MCF-7/ADR cells (IC = 0.59 μM). Additionally, compound 7a also showed great antitumor efficacy in vivo via aAsPC-1 cancer Xenograft mouse model. The preliminary mechanism study by Western blot analysis revealed that 7a repressed FAK phosphorylation in AsPC cancer cells. Taken together, the results indicate that compound 7a may serve as a promising preclinical candidate for treatment of stubborn cancers.
This article was published in the following journal.
Name: European journal of medicinal chemistry
Oral focal mucinosis an oral counterpart of cutaneous focal mucinosis, is a rare disease of unknown etiology. Its pathogenesis may be due to the overproduction of hyaluronic acid by a fibroblast, at t...
Alkoxyallylsiletanes are capable of highly chemo- and diastereoselective carbonyl allylsilylations. Reactive substrates include salicylaldehydes and glyoxylic acids. Chemoselectivity in these reaction...
The redetermination of the crystal structure of trigonal UCl6, which is the eponym for the UCl6 structure type, showed that certain atomic coordinates had been incorrectly reported. This led to notice...
The carbonyl groups of glycerolipid monolayers on water play an important role in the formation of the interfacial hydrogen bond network, which in turn influences the interactions of lipids with, for ...
Increasing availability of surgically resected brain tissue from patients with focal epilepsy and focal cortical dysplasia or low-grade glioneuronal tumors has fostered large-scale genetic examination...
Effect of Locally Delivered Antioxidants as An Adjunct to Non-surgical Periodontal Therapy on GCF Level of Oxidative Stress Marker; Protein Carbonyl
Residual renal function is reported to contribute to the survival and cardiovascular disease of peritoneal dialysis patients. Oxidative and carbonyl stress are increased in peritoneal dial...
In this study, the investigator will try to highlight the presence of carbonyl compounds in the hair follicles of women with telogen effluvium (ET) linked to stress of various origins (fat...
This is an interventional study to investigate formation and pharmacokinetics of reactive carbonyl species adducts of apple polyphenols in human after a single dose of apple consumption.
The current study aims to investigate the impact of a comprehensive, team-based, family-centered, lifestyle modification program on body weight, metabolic abnormalities, fitness measures, ...
A secondary structure of proteins that is a right-handed helix or coil, where each amino (N-H) group of the peptide backbone contributes a hydrogen bond to the carbonyl(C=O) group of the amino acid four residues N-terminal to it (n-4). It is the most common type of secondary structure.
The appearance of carbonyl groups (such as aldehyde or ketone groups) in PROTEINS as the result of several oxidative modification reactions. It is a standard marker for OXIDATIVE STRESS. Carbonylated proteins tend to be more hydrophobic and resistant to proteolysis.
Complex of iron atoms chelated with carbonyl ions.
NADPH-dependent reductase that catalyzes the reduction of many carbonyl compounds including QUINONES; PROSTAGLANDINS; and XENOBIOTICS.
A quantitative prediction of the biological, ecotoxicological or pharmaceutical activity of a molecule. It is based upon structure and activity information gathered from a series of similar compounds.
Bladder Cancer Brain Cancer Breast Cancer Cancer Cervical Cancer Colorectal Head & Neck Cancers Hodgkin Lymphoma Leukemia Lung Cancer Melanoma Myeloma Ovarian Cancer Pancreatic Cancer ...
Cancer is not just one disease but many diseases. There are more than 100 different types of cancer. Most cancers are named for the organ or type of cell in which they start - for example, cancer that begins in the colon is called colon cancer; cancer th...