The chromatographic parameters of arylpiperazinylpropyl derivatives of imidazolidine-2,4-dione and imidazo[2,1-f]purine-2,4-dione were investigated using reversed-phase thin layer chromatography method. The results revealed that R(M0) of investigated compounds depended on substituent in arylpiperazinyl fragment as well as on a nature of (cycloalkyl)aromatic ring at 5 position of imidazolidine-2,4-dione and at 7 position of imidazo[2,1-f]theophylline. The R(M0) parameters were compared with computationally calculated partition coefficients values by principal component analysis (PCA). To verify the influence of lipophilic parameter of investigated compounds on their biological activity the statistical analysis of Mann-Whitney was performed.
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Int J Biol Macromol
January 2025
Division of Cancer Research and Therapeutics (CaRT), Yenepoya Research Centre, Yenepoya (Deemed to be University), Mangalore 585018, Karnataka, India.
The current investigation intended to assess the controlled delivery of 7-sulfonamide-2-(4-methylphenyl) imidazo[2,1-b] [1, 3] benzothiazole an anticancer agent (ACA) by tamarind seed gum-based hydrogel; for its potential activity against hepatocellular carcinoma. The FTIR spectra, SEM, C NMR, PXRD, and TGA analyses evidenced the successful loading of ACA into the hydrogel system. The rheological testing conveyed the increase in the elastic nature of ACA-loaded hydrogel helping in an effective release.
View Article and Find Full Text PDFRSC Med Chem
January 2025
Fluoro-Agrochemicals, CSIR-Indian Institute of Chemical Technology Hyderabad-500 007 India
In continuation of our efforts to develop new anticancer compounds, a new series of imidazo[1,5-]pyridine-chalcone derivatives was designed, synthesized, characterized, and evaluated for its cytotoxicity against five human cancer cell lines, , breast (MDA-MB-231), colon (RKO), bone (Mg-63), prostate (PC-3), and liver (HepG2) cell lines, as well as a normal cell line (HEK). Among the synthesized compounds, two exhibited promising cytotoxicity against the MDA-MB-231 cell line with IC values of 4.23 ± 0.
View Article and Find Full Text PDFActa Crystallogr E Crystallogr Commun
January 2025
Department of Chemistry, KU Leuven, Biomolecular Architecture, Celestijnenlaan 200F, Leuven (Heverlee), B-3001, Belgium.
Two novel complexes, [Cu()Cl] and [Zn()Cl], were synthesized from 1,1'-[(3-fluoro-phen-yl)methyl-ene]bis-[3-(3-fluoro-phen-yl)imidazo[1,5-]pyridine] (), and copper(II) and zinc(II) chloride, respectively. The structures of these complexes were confirmed using ESI-MS, IR and H NMR spectra. The results reveal mononuclear structures in which the central metal atoms are coordinated by two N atoms from the imidazole rings and two Cl ligands.
View Article and Find Full Text PDFOrg Biomol Chem
January 2025
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology (ECUST), Shanghai 200237, China.
A highly efficient base-controlled synthesis of -β-trifluoromethyl-substituted 2-benzo[]imidazole-2-thiones and 2-fluoro-4-benzo[4,5]imidazo[2,1-][1,3]thiazines hydroamination or defluorinative cyclizations of α-(trifluoromethyl)styrenes with 2-mercaptobenzimidazole was developed.
View Article and Find Full Text PDFJ Fluoresc
January 2025
Department of Basic Sciences, Sari University of Agricultural Sciences and Natural Resources, P.O.Box 578, Sari, Iran.
Among the various cations, the Fe ion is one of the most critical transition metal ions in living cells for many cellular functions and enzymatic activities. The decrease or overloading of Fe can lead to different disruptions in humans. Also, Fe, highly toxic, is very common in all industrial wastewater.
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