Four classes of aminoquinoline derivatives were prepared: primaquine ureas 1a-f, primaquine bis-ureas 2a-f, chloroquine fumardiamides 3a-f and mefloquine fumardiamides 4a-f. Their antiproliferative activities against breast adeno-carcinoma (MCF-7), lung carcinoma (H460) and colon carcinoma (HCT 116 and SW620) cell lines were evaluated in vitro, using MTT cell proliferation assay. The results revealed a low activity of primaquine urea and bis-urea derivatives and high activity of all fumardiamides, with IC50 values in low micromolar range against all tested cancer cell lines.
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http://dx.doi.org/10.2478/acph-2019-0048 | DOI Listing |
Int J Mol Sci
January 2025
Department of Material Science and Engineering, College of Chemistry and Materials Science, Jinan University, Guangzhou 510632, China.
Inflammatory skin diseases comprise a group of skin conditions characterized by damage to skin function due to overactive immune responses. These disorders not only impair the barrier function of the skin but also deteriorate the quality of life and increase the risk of psychiatric issues. Here, a low-modulus phosphatidylserine-exposing microvesicle (deformed PSV, D-PSV) was produced, characterized, and evaluated for its potential therapeutic function against skin diseases.
View Article and Find Full Text PDFProc Natl Acad Sci U S A
January 2025
Cancer Biology & Genetics Program, Sloan Kettering Institute, New York, NY 10065.
Malignant peripheral nerve sheath tumors (MPNSTs) are aggressive sarcomas and the primary cause of mortality in patients with neurofibromatosis type 1 (NF1). These malignancies develop within preexisting benign lesions called plexiform neurofibromas (PNs). PNs are solely driven by biallelic loss eliciting RAS pathway activation, and they respond favorably to MEK inhibitor therapy.
View Article and Find Full Text PDFPharmaceuticals (Basel)
December 2024
Dipartimento di Scienze Biomediche Chirurgiche e Odontoiatriche, Università degli Studi di Milano, Via Pascal 36, 20133 Milano, Italy.
Four years after the COVID-19 pandemic, a very limited number of drugs has been marketed; thus, the search for new medications still represents a compelling need. In our previous work on antiviral, antiparasitic, and antiproliferative agents, we described several compounds (- and -) structurally related to clofazimine, chloroquine, and benzimidazole derivatives. Thus, we deemed it worthwhile to test them against the replication of SARS-CoV-2, together with a few other compounds (, and -), which showed some analogy to miscellaneous anti-coronavirus agents.
View Article and Find Full Text PDFMolecules
December 2024
Faculty of Pharmacy and Biochemistry, University of Zagreb, A. Kovačića 1, 10000 Zagreb, Croatia.
As the resistance of to the existing antimalarials increases, there is a crucial need to expand the antimalarial drug pipeline. We recently identified potent antimalarial compounds, namely harmiquins, hybrids derived from the β-carboline alkaloid harmine and 4-amino-7-chloroquinoline, a key structural motif of chloroquine (CQ). To further explore the structure-activity relationship, we synthesised 13 novel hybrid compounds at the position -9 of the β-carboline ring and evaluated their efficacy in vitro against 3D7 and Dd2 strains (CQ sensitive and multi-drug resistant, respectively).
View Article and Find Full Text PDFMolecules
December 2024
Laboratorio de Química Inorgánica y Organometálica, Departamento de Química Analítica e Inorgánica, Facultad de Ciencias Químicas, Universidad de Concepción, Edmundo Larenas 129, Casilla 160-C, Concepción 4070386, Chile.
Organic compounds with 1,3-diketone or 3-amino enone functional groups are extremely important as they can be converted into a plethora of carbo- or heterocyclic derivatives or can be used as ligands in the formation of metal complexes. Here, we have achieved the preparation of a series of non-symmetrical β-ketoenamines (O,N,N proligand) of the type (4-MeOCH)C(=O)CH=C(R)NH(Q) obtained through the Schiff base condensation of 1,3-diketones (1-anisoylacetone, 1-anisyl-3-(4-cyanophenyl)-1,3-propanedione, and 1-anisyl-3-(4,4,4-trifluorotolyl)-1,3-propanedione) functionalized with electron donor and electron-withdrawing substituents and 8-aminoquinoline (R = CH, 4-CHCN, 4-CHCF; Q = CHN). Schiff base ketoimines with a pendant quinolyl moiety were isolated as single regioisomers in yields of 22-56% and characterized with FT-IR, H NMR, and UV-visible spectroscopy, as well as single-crystal X-ray crystallography, which allowed for the elucidation of the nature of the isolated regioisomers.
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