The synthesis of several monomeric and dimeric steroidal [1,2,4]triazolo[1,5-a]pyrimidines (TPs) derived from steroids are described. These derivatives were prepared from α,β-unsaturated carbonyl compounds through a Claisen Schmidt condensation and rearrangement of the spiro moiety followed by a cycloaddition with 3-amino-1,2,4-triazole. The antiproliferative activity of compounds 7, 13-15 was tested against human cancer cells; several IG values were below 10μM.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.steroids.2016.09.014 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Calcium phosphate formation and deposition in ischemic neurons.
PLoS One
January 2025
Biomedical Engineering Department, Northwestern University, Evanston, IL, United States of America.
Ischemic stroke causes acute brain calcium phosphate (CaP) deposition, a process involving primarily the injured neurons. Whereas the adverse impact of CaP deposition on the brain structure and function has been recognized, the underlying mechanisms remain poorly understood. This investigation demonstrated that the neuron-expressed, plasma membrane-associated Ca2+-binding proteins annexin (Anx) A2, AnxA5, AnxA6, and AnxA7 contributed to neuronal CaP deposition in the mouse model of ischemic stroke.
View Article and Find Full Text PDFOsteoporosis (OP) is a prevalent metabolic bone disease globally. Currently, the development of Traditional Chinese Medicine (TCM) resources to unblock joints, strengthen bones, and enhance muscle function to regulate anti-osteogenic and anabolic metabolism and thus reshape intraosseous homeostasis was an effective way to alleviate OP. The F-E-D formula, comprising Fructus Psoraleae, Eucommia, and Drynariae Rhizoma, has shown efficacy in treating OP.
View Article and Find Full Text PDFControl of HS synthesis by the monomer-oligomer transition of OsCBSX3 for modulating rice growth-immunity balance.
Mol Plant
January 2025
State Key Laboratory of Wheat Improvement, Shandong Provincial Key Laboratory of Agricultural Microbiology, College of Plant Protection, Shandong Agricultural University, Tai'an 271018, China. Electronic address:
Hydrogen sulfide (H2S) is recognized as an important gaseous signaling molecule, similar to nitric oxide and carbon monoxide. However, the synthesis mechanism of H2S and its role in enhancing rice resistance to Xanthomonas oryzae pv. oryzicola (Xoc) and Xanthomonas oryzae pv.
View Article and Find Full Text PDFThe small GTPase MRAS is a broken switch.
Nat Commun
January 2025
Institute for Research in Immunology and Cancer (IRIC), Université de Montréal, Montréal, QC, H3T 1J4, Canada.
Intense research on founding members of the RAS superfamily has defined our understanding of these critical signalling proteins, leading to the premise that small GTPases function as molecular switches dependent on differential nucleotide loading. The closest homologs of H/K/NRAS are the three-member RRAS family, and interest in the MRAS GTPase as a regulator of MAPK activity has recently intensified. We show here that MRAS does not function as a classical switch and is unable to exchange GDP-to-GTP in solution or when tethered to a lipid bilayer.
View Article and Find Full Text PDFScutellarein Inhibits Osteosarcoma Growth by Targeting the TLR4/TRAF6/NF-κB Pathway.
Drug Des Devel Ther
January 2025
Department of Trauma Orthopedics, Affiliated Hospital of Jining Medical University, Jining, Shandong, 272007, People's Republic of China.
Purpose: Osteosarcoma (OS) is the most common malignant tumor associated with poor patient outcomes and a limited availability of therapeutic agents. Scutellarein (SCU) is a monomeric flavone bioactive compound with potent anti-cancer activity. However, the effects and mechanisms of SCU on the growth of OS remain unknown.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!