Rucaparib and PJ34 were used as the structural model for the design of novel 5H-dibenzo[b,e]azepine-6,11-dione derivatives containing 1,3,4-oxadiazole units. And target compounds were successfully synthesized through a 3-step synthetic strategy. All target compounds were screened for their anti-proliferative effects against OVCAR-3 cell line. Preliminary biological study of these compounds provided potent compounds d21 and d22 with better activities than Rucaparib.
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http://dx.doi.org/10.1016/j.bmcl.2018.02.008 | DOI Listing |
Proc Natl Acad Sci U S A
August 2024
Department of Neurology, The David Geffen School of Medicine at University of California Los Angeles, Los Angeles, CA 90095.
Brain rhythms provide the timing for recruitment of brain activity required for linking together neuronal ensembles engaged in specific tasks. The γ-oscillations (30 to 120 Hz) orchestrate neuronal circuits underlying cognitive processes and working memory. These oscillations are reduced in numerous neurological and psychiatric disorders, including early cognitive decline in Alzheimer's disease (AD).
View Article and Find Full Text PDF3 Biotech
March 2024
MS Swaminathan School of Agriculture, Shoolini University of Biotechnology and Management Sciences, Bajhol, Solan, Himachal Pradesh 173229 India.
Bioactive compounds in plants are essential for the formation of novel chemotherapeutic drugs, which have been used in Ayurveda to treat a variety of illnesses. Indian medicinal herbs have been used for thousands of years to treat a variety of illnesses, such as fever, cancer, snake bites, rheumatism, skin problems, and neurodegenerative diseases. GC-MS was used to locate and categorize bioactive components in leaves.
View Article and Find Full Text PDFBeilstein J Org Chem
January 2024
LAQV-REQUIMTE, University of Évora, Rua Romão Ramalho, 59, 7000 Évora, Portugal.
A sequential strategy to access 10,11-dihydro-5-dibenzo[,][1,4]diazepinones (DBDAPs) is disclosed in this article through a palladium and copper-catalyzed amination (Buchwald-Hartwig (B-H) or Chan-Lam (C-L)) followed by a palladium-catalyzed intramolecular aminocarbonylation with Mo(CO) as CO surrogate (to avoid toxic CO handling) of readily available -phenylenediamines and either 1,2-dibromobenzene or 2-bromophenylboronic acid. The 10,11-dihydro-5-dibenzo[,][1,4]diazepinone could be synthezised in good yield using a sequential catalytic procedure, using both C-L and B-H approaches. Gratifingly, the use of the C-L reaction was more impressive, and afforded the dibenzodiazepinones in good yields (up to 45%; 2 steps) and much milder conditions using copper as the catalyst.
View Article and Find Full Text PDFRSC Adv
October 2021
State Key Laboratory of Fine Chemicals, Dalian University of Technology Dalian 116024 P. R. China
A novel 3D lanthanide(iii) metal-organic framework (MOF) (namely Tb-MOF), was synthesized by self-assembly from Tb(iii) ion nitrate and the rigid organic ligand Hsbdc (Hsbdc = 5,5-dioxo-5-dibenzo[,]thiophene-3,7-dicarboxylic acid), and could work as an efficient heterogeneous catalyst for the cyanosilylation of aromatic aldehydes at room temperature. The obtained Tb-MOF has been characterized and analysed in detail by single crystal X-ray diffraction, powder X-ray diffraction, thermogravimetric analysis and so on. The pores of Tb-MOF provided a microenvironment that was beneficial for the substrates to be close to the Lewis acid catalytic sites.
View Article and Find Full Text PDFInorg Chem
February 2022
State Key Laboratory of Fine Chemicals, Zhang Dayu School of Chemistry, Dalian University of Technology, Dalian 116024, China.
Adenosine triphosphate (ATP) is an important kind of metabolized biological molecule that is formed in organisms, especially in mitochondria, is used universally as energy, and is one of the most significant multifunctional biological molecules. Metal-organic frameworks (MOFs) have been widely used in many applications such as gas storage and separation, drug delivery, heterogeneous catalysis, chemical sensors, etc. Remarkably, lanthanide MOFs (Ln-MOFs), which display large pores, multiple dimensions, and unique lanthanide luminescence properties, are widely used as chemical sensors.
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