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Anticancer activity of novel 3-(furan-2-yl)pyrazolyl and 3-(thiophen-2-yl)pyrazolyl hybrid chalcones: Synthesis and in vitro studies.
Helmy, Mirna T; Sroor, Farid M; Mahrous, Karima F; Mahmoud, Khaled; Hassaneen, Hamdi M; Saleh, Fatma M; Abdelhamid, Ismail A; Mohamed Teleb, Mohamed A.
Afiliación
  • Helmy MT; Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt.
  • Sroor FM; Organometallic and Organometalloid Chemistry Department, National Research Centre, Cairo, Egypt.
  • Mahrous KF; Institut für Anorganische Chemie, Universität Göttingen, Göttingen, Germany.
  • Mahmoud K; Cell Biology Department, National Research Centre, Dokki, Egypt.
  • Hassaneen HM; Pharmacognosy Department, National Research Centre, Dokki, Egypt.
  • Saleh FM; Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt.
  • Abdelhamid IA; Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt.
  • Mohamed Teleb MA; Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt.
Arch Pharm (Weinheim) ; 355(3): e2100381, 2022 Mar.
Article en En | MEDLINE | ID: mdl-34939695
Twelve novel chalcone derivatives were prepared using the Claisen-Schmidt condensation reaction. The reaction of 4-acetyl-5-furan/thiophene-pyrazole derivatives 5 with the corresponding aldehydes 6 afforded the targeted chalcone derivatives 7a-l in good yields. The newly synthesized chalcones were fully characterized by spectrometric and elemental analyses. The in vitro anticancer activities of the novel compounds 7a-l were evaluated against four human cancer cell lines: HepG2 (human hepatocellular carcinoma), MCF7 (human Caucasian breast adenocarcinoma), A549 (lung carcinoma), and BJ1 (normal skin fibroblasts). Compound 7g emerged as the most promising compound, with IC50 = 27.7 µg/ml against A549 cells compared to the reference drug doxorubicin (IC50 = 28.3 µg/ml), and IC50 = 26.6 µg/ml against HepG2 cells compared to the reference drug doxorubicin (IC50 = 21.6 µg/ml). The gene expression and DNA damage values and the DNA fragmentation percentages for compound 7g were determined on the lung and liver cell lines. The expression levels of the AMY2A and FOXG1 genes increased significantly (p < 0.01) in the negative samples of lung cancer cells compared with treated cells. Also, the expression values of the PKM and PSPH genes improved significantly (p < 0.01) in the negative samples compared with treated samples of liver cancer cells. The DNA damage values increased significantly (p < 0.01) in treated lung cell line samples (7g) and the positive control. The results showed a significant decrease (p < 0.05) in DNA damage values in the negative samples of liver cancer cells compared to those treated with 7g. However, the DNA fragmentation values increased significantly (p < 0.01) in the treated lung and liver cell line samples compared with the negative control.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Chalcona / Chalconas / Antineoplásicos Límite: Humans Idioma: En Revista: Arch Pharm (Weinheim) Año: 2022 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Alemania
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Chalcona / Chalconas / Antineoplásicos Límite: Humans Idioma: En Revista: Arch Pharm (Weinheim) Año: 2022 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Alemania