This study describes a one-pot photoinduced method for azepine synthesis and their subsequent rearrangement into pyridines. The rearrangement of the azepine, formed during photolysis, occurs due to both thermal and photochemical activation of the reaction. This requires an electron-donating substituent at the second position of the azepine and an electron-withdrawing substituent at the third position of the azepine. A reaction mechanism has been proposed to explain the role of water and the nature of the azepine substituents.
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http://dx.doi.org/10.1021/acs.joc.3c01453 | DOI Listing |
ACS Chem Biol
November 2024
Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
Synthetic genome readers/regulators (SynGRs) are bifunctional molecules that are rationally designed to bind specific genomic sequences and engage cellular machinery that regulates the expression of targeted genes. The prototypical SynGR1 targets GAA trinucleotide repeats and recruits the BET family of transcriptional regulatory proteins via a flexibly tethered ligand, JQ1. This pan-BET ligand binds both tandem bromodomains of BET proteins (BD1 and BD2).
View Article and Find Full Text PDFBioorg Chem
October 2024
Organic and Medicinal Chemistry Division, CSIR-Indian Institute of Chemical Biology, 4, Raja S. C. Mullick Road, Kolkata 700032, India. Electronic address:
An unprecedented metal-free synthesis of fused quinoxaline 1,5-disubstituted-[1,4]-diazepine hybrids have been reported under mild conditions through a domino intermolecular SAr followed by an internal nucleophile-triggered intramolecular SAr pathway. Our strategy offers the flexibility for the introduction of a broad variety of functionalities at the N-1 position of fused diazepine moiety by using suitable diamine tails to design structurally diverse scaffolds. The DNA binding properties of representative quinoxaline diazepine hybrids were studied using UV-vis absorbance and EtBr displacement assay and were found to be governed by the functionalities at the N-1 position.
View Article and Find Full Text PDFCancer Lett
January 2025
Translational and Functional Genomics Branch, National Human Genome Research Institute, Bethesda, MD, 20892, USA. Electronic address:
Ovarian cancer, a significant contributor to cancer-related mortality, exhibits limited responsiveness to hormonal therapies targeting the estrogen receptor (ERα). This study aimed to elucidate the mechanisms behind ERα resistance to the therapeutic drug Fulvestrant (ICI182780 or ICI). Notably, compared to the cytoplasmic version, nuclear ERα was minimally degraded by ICI, suggesting a mechanism for drug resistance via the protective confines of the nuclear substructures.
View Article and Find Full Text PDFWaste Manag
October 2024
Department of Chemical Engineering, Konkuk University, 120 Neungdong-ro, Gwangjin-gu, Seoul 05029, Republic of Korea. Electronic address:
Here we report a novel chemical recycling of carbon fiber-reinforced plastic (CFRP) using meta-chloroperoxybenzoic acid (mCPBA) as the representative oxidizing agent. The optimal decomposition conditions for the epoxy (EP) resin in CFRP were investigated by varying mCPBA concentration and reaction time. The CFRP decomposed completely within 6 h using a 1.
View Article and Find Full Text PDFEpilepsia Open
August 2024
Department of Neurology, The Affiliated Hospital of Zunyi Medical University, Zunyi, China.
Objective: The objective of this study is to determine whether inhibition of mitophagy affects seizures through Clathrin-mediated endocytosis (CME).
Methods: Pentylenetetrazol (PTZ) was intraperitoneally injected daily to establish a chronic PTZ-kindled seizure. The Western blot (WB) was used to compare the differences in Parkin protein expression between the epilepsy group and the control group.
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