Browsing by Author "Abdelhamid, Ismail A"

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Chalcones: Promising therapeutic agents targeting key players and signaling pathways regulating the hallmarks of cancer
(Elsevier Ireland Ltd, 2023-01) WalyEldeen, Amr Ahmed,; Sabet, Salwa; El-Shorbagy, Haidan M.; Abdelhamid, Ismail A; Ibrahim, Sherif Abdelaziz
The need for innovative anticancer treatments with high effectiveness and low toxicity is urgent due to the development of malignancies that are resistant to chemotherapeutic agents and the poor specificity of existing anticancer treatments. Chalcones are 1,3-diaryl-2-propen-1-ones, which are the precursors for flavonoids and isoflavonoids. Chalcones are readily available from a wide range of natural resources and consist of very basic chemical scaffolds. Because the ease with which the synthesis it allows for the production of several chalcone derivatives. Various in-vitro and in-vivo studies indicate that naturally occurring and synthetic chalcone de- rivatives exhibit promising biological activities against cancer hallmarks such as proliferation, angiogenesis, invasion, metastasis, inflammation, stemness, and regulation of cancer epigenetics. According to their structure and functional groups, chalcones derivatives and their hybrid compounds exert a broad range of biological ac- tivities through targeting key elements and signaling molecules relevant to cancer progression. This review will provide valuable insights into the latest updates of chalcone groups as anticancer agents and extensively discuss their underlying molecular mechanisms of action.
Synthesis, anticancer evaluation of novel hybrid pyrazole-based chalcones, molecular docking, DNA fragmentation, and gene expression: in vitro studies
(Royal Society of Chemistry, 2024-07) Yasser, Norhan; Sroor, Farid M; El-Shorbagy, Haidan M; Eissa, Shaymaa M; Abdelhamid, Ismail A; Hassaneen, Hamdi M
A unique series of pyrazolyl-chalcone derivatives was synthesized via the method of Claisen-Schmidt condensation. The desired chalcone derivatives 7a-d and 9a-f were obtained in good yields by reacting the 4-acetyl-5-thiophene-pyrazole with the appropriate heteroaryl aldehyde derivatives. The novel chalcones have undergone complete elemental analysis, 1H-NMR, 13C-NMR, mass spectrometry, and IR characterization. The three human cancer cell lines MCF7 (human Caucasian breast adenocarcinoma), PC3 (prostatic cancer) and PACA2 (pancreatic carcinoma) as well as the normal cell line BJ1 (normal skin fibroblasts) were tested in vitro for the anti-cancer properties of the newly synthesized chalcone derivatives. When compared to the reference medicine doxorubicin (IC50 = 52.1 μM), compound 9e showed the most promise derivative (IC50 = 27.6 μM) against PACA2 cells, while compound 7d demonstrated anticancer efficacy (IC50 = 42.6 μM against MCF7 cells compared to the reference drug doxorubicin (IC50 = 48 μM). Using breast and pancreatic cell lines, the gene expression, DNA damage, and DNA fragmentation percentages for compounds 7d and 9e were evaluated. Moreover, the molecular docking study of compounds 7d and 9e was assessed. The binding affinities of compound 9e toward P53 mutant Y220C was −22 kcal per mole, while those of compound 7d towards Bcl2 and CDK4 were −27.81 and −26.9 kcal per mole, respectively, compared to the standard values (−15.82, −33.96 and −29.9 kcal per mole).
Synthesis, anticancer evaluation of novel hybrid pyrazole-based chalcones, molecular docking, DNA fragmentation, and gene expression: in vitro studies
(Royal Society of Chemistry, 2024-07) Yasser, Norhan; Sroor, Farid M; El-Shorbagy, Haidan M; Eissa, Shaymaa M; Abdelhamid, Ismail A; Hassaneen, Hamdi M
A unique series of pyrazolyl-chalcone derivatives was synthesized via the method of Claisen-Schmidt condensation. The desired chalcone derivatives 7a-d and 9a-f were obtained in good yields by reacting the 4-acetyl-5-thiophene-pyrazole with the appropriate heteroaryl aldehyde derivatives. The novel chalcones have undergone complete elemental analysis, 1H-NMR, 13C-NMR, mass spectrometry, and IR characterization. The three human cancer cell lines MCF7 (human Caucasian breast adenocarcinoma), PC3 (prostatic cancer) and PACA2 (pancreatic carcinoma) as well as the normal cell line BJ1 (normal skin fibroblasts) were tested in vitro for the anti-cancer properties of the newly synthesized chalcone derivatives. When compared to the reference medicine doxorubicin (IC50 = 52.1 μM), compound 9e showed the most promise derivative (IC50 = 27.6 μM) against PACA2 cells, while compound 7d demonstrated anticancer efficacy (IC50 = 42.6 μM against MCF7 cells compared to the reference drug doxorubicin (IC50 = 48 μM). Using breast and pancreatic cell lines, the gene expression, DNA damage, and DNA fragmentation percentages for compounds 7d and 9e were evaluated. Moreover, the molecular docking study of compounds 7d and 9e was assessed. The binding affinities of compound 9e toward P53 mutant Y220C was −22 kcal per mole, while those of compound 7d towards Bcl2 and CDK4 were −27.81 and −26.9 kcal per mole, respectively, compared to the standard values (−15.82, −33.96 and −29.9 kcal per mole).