The condensation reaction of diphenylamine with 2-oxo-2H-(substituted chromen)-4-yl acetic acid in presence of anhydrous zinc chloride afford 4-(acridine-9-ylmethyl)-2H-(substituted chromen)-2-one. The synthesized compounds were characterized by spectral studies and elemental analysis and screened for their in vitro antibacterial activity against Staphylococcus aureus, Staphylococcus pyogenes (gram +ve), Escherichia coli, Pseudomonas aeruginosa (gram -ve) and antifungal activity against Aspergillus niger and anticancer activity (HL-60, Hep-2 & HEK293T) by MTT assay. Chloro substituted compounds showed antimicrobial and anticancer activity with IC(50) values in the low micromolar range.
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http://dx.doi.org/10.1016/j.bmcl.2010.06.001 | DOI Listing |
Chem Biodivers
December 2024
Department of Biochemistry, Government College Women University, Faisalabad, Pakistan.
The current study was conducted to characterize the vinegar extract of Nigella sativa and evaluate its biological activities using in vitro and in vivo studies. The N. sativa extract (NSE) was prepared by macerating seeds in a mixture of water and synthetic vinegar (1:10).
View Article and Find Full Text PDFDiscov Oncol
January 2025
Graduate School of Qinghai University, Xining, 810000, Qinghai Province, People's Republic of China.
The occurrence and progression of breast cancer (BCa) are complex processes involving multiple factors and multiple steps. The tumor microenvironment (TME) plays an important role in this process, but the functions of immune components and stromal components in the TME require further elucidation. In this study, we obtained the RNA-seq data of 1086 patients from The Cancer Genome Atlas (TCGA) database.
View Article and Find Full Text PDFDalton Trans
January 2025
Institute of Biopharmaceutical Research, Liaocheng University, Liaocheng 252059, P. R. China.
Pt(IV) complexes as prodrugs of Pt(II) drugs exhibit numerous advantages such as enhanced stability, reduced toxicity, increased oral bioavailability, and efficacy in overcoming the drug resistance of Pt(II) compounds, which underscore their significant potential in the advancement of novel Pt anticancer agents. Furthermore, protective autophagy is pivotal in sustaining tumor cell homeostasis and modulating the tumor microenvironment (TME), thereby representing a critical target for the development of antitumor drugs. Specific inhibition or activation of autophagy during chemotherapy would break the internal homeostasis in the TME and increase antitumor activities.
View Article and Find Full Text PDFJ Med Chem
January 2025
Key Laboratory of Protection, Development and Utilization of Medicinal Resources in Liupanshan Area, Ministry of Education, School of Pharmacy, Ningxia Medical University, 1160 Shengli Street, Yinchuan, Ningxia Province 750004, China.
Genetic mutations in components of the Hippo pathway frequently lead to the aberrant activation of TEADs, which is often associated with cancer. Consequently, TEADs have been actively pursued as therapeutic targets for diseases driven by TEAD overactivation. In this study, we report two series of TEAD PROTACs based on CRBN binders and VHL binders.
View Article and Find Full Text PDFChem Rec
January 2025
Department of Pharmacy, Banasthali Vidyapith, Rajasthan, India.
Seven-membered nitrogen-containing heterocycles, particularly azepine-based compounds, represent an intriguing class of molecules with vast arrays of applications. These compounds have garnered considerable attention in synthetic and medicinal chemistry due to their non-planar, non-aromatic features, which offer structural flexibility and diversity to design new drugs with improved pharmacological properties. This review summarizes the recent advances in the synthesis of azepine derivatives, including eco-friendly methodologies that align with the principles of green chemistry, which emphasize atom economy, sustainability, and waste reduction.
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