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Design, Synthesis, Antitumor, and Antiplasmodial Evaluation of New 7-Chloroquinoline-Benzimidazole Hybrids.
Krstulovic, Luka; Rastija, Vesna; Pessanha de Carvalho, Lais; Held, Jana; Rajic, Zrinka; Zivkovic, Zorislava; Bajic, Miroslav; Glavas-Obrovac, Ljubica.
Afiliación
  • Krstulovic L; Department of Chemistry and Biochemistry, Faculty of Veterinary Medicine, University of Zagreb, Heinzelova 55, HR-10000 Zagreb, Croatia.
  • Rastija V; Department of Agroecology and Environmental Protection, Faculty of Agrobiotechnical Sciences Osijek, Josip Juraj Strossmayer University of Osijek, Vladimira Preloga 1, HR-31000 Osijek, Croatia.
  • Pessanha de Carvalho L; Institute of Tropical Medicine, University of Tuebingen, Wilhelmstrasse 27, D-72074 Tuebingen, Germany.
  • Held J; Institute of Tropical Medicine, University of Tuebingen, Wilhelmstrasse 27, D-72074 Tuebingen, Germany.
  • Rajic Z; Partner Site Tuebingen, German Center for Infection Research (DZIF),Wilhelmstrasse 27, D-72074 Tuebingen, Germany.
  • Zivkovic Z; Department of Medicinal Chemistry, Faculty of Pharmacy and Biochemistry, University of Zagreb, A. Kovacica 1, HR-10000 Zagreb, Croatia.
  • Bajic M; General County Hospital of Nasice, Bana Jelacica 10, HR-31500 Nasice, Croatia.
  • Glavas-Obrovac L; Department of Chemistry and Biochemistry, Faculty of Veterinary Medicine, University of Zagreb, Heinzelova 55, HR-10000 Zagreb, Croatia.
Molecules ; 29(13)2024 Jun 24.
Article en En | MEDLINE | ID: mdl-38998949
ABSTRACT
Newly synthesized 7-chloro-4-aminoquinoline-benzimidazole hybrids were characterized by NMR and elemental analysis. Compounds were tested for their effects on the growth of the non-tumor cell line MRC-5 (human fetal lung fibroblasts) and carcinoma (HeLa and CaCo-2), leukemia, and lymphoma (Hut78, THP-1, and HL-60) cell lines. The obtained results, expressed as the concentration at which 50% inhibition of cell growth is achieved (IC50 value), show that the tested compounds affect cell growth differently depending on the cell line and the applied dose (IC50 ranged from 0.2 to >100 µM). Also, the antiplasmodial activity of these hybrids was evaluated against two P. falciparum strains (Pf3D7 and PfDd2). The tested compounds showed potent antiplasmodial activity, against both strains, at nanomolar concentrations. Quantitative structure-activity relationship (QSAR) analysis resulted in predictive models for antiplasmodial activity against the 3D7 strain (R2 = 0.886; Rext2 = 0.937; F = 41.589) and Dd2 strain (R2 = 0.859; Rext2 = 0.878; F = 32.525) of P. falciparum. QSAR models identified the structural features of these favorable effects on antiplasmodial activities.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Plasmodium falciparum / Bencimidazoles / Diseño de Fármacos / Relación Estructura-Actividad Cuantitativa / Antimaláricos / Antineoplásicos Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2024 Tipo del documento: Article País de afiliación: Croacia Pais de publicación: Suiza
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Plasmodium falciparum / Bencimidazoles / Diseño de Fármacos / Relación Estructura-Actividad Cuantitativa / Antimaláricos / Antineoplásicos Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2024 Tipo del documento: Article País de afiliación: Croacia Pais de publicación: Suiza