The present review offers an apt summary of amide bond formation with carboxylic acid substrates by taking advantage of several methods. Carboxamides can be regarded as a substantial part of organic and medicinal chemistry due to their utility in synthesizing peptides, lactams, and more than 25% of familiar drugs. Moreover, they play a leading role in the synthesis of bioactive products with anticancer, antifungal, and antibacterial properties. The data are arranged based on the type and amount of reagents used to conduct amidation and are also divided into the following categories: catalytic amidation of carboxylic acids, non-catalytic amidation, and transamidation.
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http://dx.doi.org/10.1007/s11030-021-10252-0 | DOI Listing |
J Biol Chem
September 2024
Laboratory of Cell and Developmental Signaling, Center for Cancer Research, National Cancer Institute at Frederick, NIH, Frederick, Maryland, USA. Electronic address:
NXP900 is a selective and potent SRC family kinase (SFK) inhibitor, currently being dosed in a phase 1 clinical trial, that locks SRC in the "closed" conformation, thereby inhibiting both kinase-dependent catalytic activity and kinase-independent functions. In contrast, several multi-targeted kinase inhibitors that inhibit SRC, including dasatinib and bosutinib, bind their target in the active "open" conformation, allowing SRC and other SFKs to act as a scaffold to promote tumorigenesis through non-catalytic functions. NXP900 exhibits a unique target selectivity profile with sub-nanomolar activity against SFK members over other kinases.
View Article and Find Full Text PDFMol Oncol
August 2024
Institute of Toxicology, University Medical Center of the Johannes Gutenberg University Mainz, Mainz, Germany.
Mammalian cells replicate ~ 3 × 10 base pairs per cell cycle. One of the key molecules that slows down the cell cycle and prevents excessive DNA damage upon DNA replication stress is the checkpoint kinase ataxia-telangiectasia-and-RAD3-related (ATR). Proteolysis-targeting-chimeras (PROTACs) are an innovative pharmacological invention to molecularly dissect, biologically understand, and therapeutically assess catalytic and non-catalytic functions of enzymes.
View Article and Find Full Text PDFJ Mater Chem B
August 2023
Petrochemical Technology and Industrial Ecology Department, Azerbaijan State Oil and Industry University, Baku, AZ 1010, Azerbaijan.
This study is devoted to the synthesis of a 40-membered macroheterocycle with its further nanostructuring by magnetite nanoparticles. The mentioned macroheterocycle was synthesized by the [2+2] cyclocondensation of the oxygen-containing diamine with an aromatic dialdehyde in a non-catalytic medium and with no work-up procedure. The structure of the obtained macroheterocycle was studied by H and C nuclear magnetic resonance spectroscopy and matrix-assisted laser desorption/ionization-time of flight mass spectrometry.
View Article and Find Full Text PDFInt J Mol Sci
June 2023
Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Science, Arbuzova Str., 8, Kazan 420088, Russia.
Herein, we report the design and synthesis of novel 7-aza-coumarine-3-carboxamides via scaffold-hopping strategy and evaluation of their in vitro anticancer activity. Additionally, the improved non-catalytic synthesis of 7-azacoumarin-3-carboxylic acid is reported, which features water as the reaction medium and provides a convenient alternative to the known methods. The anticancer activity of the most potent 7-aza-coumarine-3-carboxamides against the HuTu 80 cell line is equal to that of reference Doxorubicin, while the selectivity towards the normal cell line is 9-14 fold higher.
View Article and Find Full Text PDFChemosphere
September 2023
College of Environmental and Resource Sciences, Zhejiang University, Hangzhou, 320058, China. Electronic address:
The molecular nest structured catalysts have demonstrated better performance than the traditional supported catalysts. However, they have not been tried in antibiotics or other organic pollutants removal from water by advanced oxidation processes (AOPs). Here we synthesized Mn anchored zeolite molecular nest (Mn@ZN) for the catalytic ozonation of cephalexin (CLX), which is the widely used antibiotic and also a refractory pollutant in water.
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