[reaction: see text] A recently discovered multicomponent coupling reaction is used to give direct access to a late intermediate in the synthesis of frondosin B. This intermediate can also be efficiently converted to a ring-expanded analogue of frondosin B by sustained heating of the reaction mixture. An unprecedented tandem 1,7-hydrogen shift, 8pi-electrocyclization is proposed to explain the formation of this ring-expanded species.
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http://dx.doi.org/10.1021/ol035822q | DOI Listing |
Comb Chem High Throughput Screen
January 2025
APIGENEX s.r.o., Poděbradská 173/5, Prague 19000, Czech Republic.
Objective: In search of efficient anticancer agents, we aimed at the design and synthesis of a library of tetrasubstituted alkenes. These are structural analogues of tamoxifen, one of the widely used anticancer therapeutics.
Methods: Our small organic compound library was prepared via a chemical synthesis in the solution using the Larock three-component coupling reaction, which is known to tolerate diverse functional groups.
Bioorg Med Chem Lett
January 2025
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 100049, China; School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou 310024, China. Electronic address:
The discovery of novel anticancer agents remains a critical goal in medicinal chemistry, with innovative synthetic methodologies playing a pivotal role in advancing this field. Recent breakthroughs in CH activation reactions, cyclization reactions, multicomponent reactions, cross-coupling reactions, and photo- and electro-catalytic reactions have enabled the efficient synthesis of new molecular scaffolds exhibiting potent biological activities, including anticancer properties. These methodologies have facilitated the functionalization of natural products, the modification of bioactive molecules, and the generation of entirely new compounds, many of which demonstrate strong antitumor activity.
View Article and Find Full Text PDFMaterials (Basel)
December 2024
Shanghai Frontiers Science Research Center of Advanced Textiles, Engineering Research Center of Technical Textiles (Ministry of Education), Key Laboratory of Textile Science & Technology (Ministry of Education), College of Textiles, Donghua University, Shanghai 201620, China.
Microwave absorbers with infrared camouflage are highly desirable in military fields. Self-supporting 3D architectures with tailorable shapes, composed of FeCoNi alloy/carbon nanotubes (CNTs) @ carbon nanofibers (CNFs), were fabricated in this study. On the one hand, multiple loss mechanisms were introduced into the high-elastic sponges.
View Article and Find Full Text PDFMolecules
December 2024
Institut für Pharmazeutische und Medizinische Chemie, Universität Münster, Corrensstraße 48, D-48149 Münster, Germany.
The serine/threonine kinase CK2 (formerly known as casein kinase II) plays a crucial role in various CNS disorders and is highly expressed in various types of cancer. Therefore, inhibiting this key kinase could be promising for the treatment of these diseases. The CK2 holoenzyme is formed by the recruitment of two catalytically active CK2α and/or CK2α' subunits by a regulatory CK2β dimer.
View Article and Find Full Text PDFAnal Chem
January 2025
Key Laboratory of Laboratory Medicine, Ministry of Education, Zhejiang Provincial Key Laboratory of Medical Genetics, Cixi Biomedical Research Institute, School of Laboratory Medicine and Life sciences, Wenzhou Medical University, Wenzhou 325035, China.
Accurate identification of cancer cells under complex physiological environments holds great promise for noninvasive diagnosis and personalized medicine. Herein, we developed dual-aptamer-based DNA logic-gated series lamp probes (Apt-SLP) by coupling a DNA cell-classifier (DCC) with a self-powered signal-amplifier (SSA), enabling rapid and sensitive identification of cancer cells in a blood sample. DCC is endowed with two extended-aptamer based modules for recognizing the two cascade cell membrane receptors and serves as a DNA logic gate to pinpoint a particular and narrow subpopulation of cells from a larger population of similar cells.
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