Synthesis of Bioactive Phthalazine-Coumarin Conjugates as Promising Anticancer Agents
El-Bery, E., Abo Elsoud, E., Awad, H., Tantawy, I., Abdel Bary, H., O. Khalil, F., Mohamady, M. (2025). Synthesis of Bioactive Phthalazine-Coumarin Conjugates as Promising Anticancer Agents. EKB Journal Management System, (), -. doi: 10.21608/ejchem.2025.419575.12294
Esraa Nazieh El-Bery; Esraa Fahmy Abo Elsoud; Hanem Awad; Ibrahim Tantawy; Hamed Abdel Bary; Fatma O. Khalil; Mohamed Mohamady. "Synthesis of Bioactive Phthalazine-Coumarin Conjugates as Promising Anticancer Agents". EKB Journal Management System, , , 2025, -. doi: 10.21608/ejchem.2025.419575.12294
El-Bery, E., Abo Elsoud, E., Awad, H., Tantawy, I., Abdel Bary, H., O. Khalil, F., Mohamady, M. (2025). 'Synthesis of Bioactive Phthalazine-Coumarin Conjugates as Promising Anticancer Agents', EKB Journal Management System, (), pp. -. doi: 10.21608/ejchem.2025.419575.12294
El-Bery, E., Abo Elsoud, E., Awad, H., Tantawy, I., Abdel Bary, H., O. Khalil, F., Mohamady, M. Synthesis of Bioactive Phthalazine-Coumarin Conjugates as Promising Anticancer Agents. EKB Journal Management System, 2025; (): -. doi: 10.21608/ejchem.2025.419575.12294

Synthesis of Bioactive Phthalazine-Coumarin Conjugates as Promising Anticancer Agents

Egyptian Journal of Chemistry
Articles in Press, Accepted Manuscript, Available Online from 17 November 2025
Document Type: Original Article
DOI: 10.21608/ejchem.2025.419575.12294
Authors
Esraa Nazieh El-Bery1; Esraa Fahmy Abo Elsoud1; Hanem Awad2; Ibrahim Tantawy* 3; Hamed Abdel Bary4; Fatma O. Khalil5; Mohamed Mohamady6
1Department of Chemistry, Faculty of Science, Menoufia University, Shebin El-Kom 32511, Menoufia, Egypt;
2Tanning Materials and Leather Technology Department, National Research Centre, Egypt
3Department of Chemistry, Faculty of Science, Menoufia University, Shebin El-Kom, Egypt.
4Faculty of Science, Menoufia University
5National Liver Institute, Menoufia University
6Pathology department National liver institute hospital menoufia university, Shebin Elkom, 32511, Menoufia Egypt
Abstract
Newly synthesized phthalazine-coumarin hybrids 6a-g were synthesized via amination of 4- toluyl -1-toluyl phthalazine 1 with various diamines 2a-g to form the bis amino phthalazine 3a-g, further coupling of 3a-g with coumarin-3-acetyl chloride 5 afford phthalazine-coumarin hybrids 6a-g. The installation of hybrids was confirmed by spectroscopic methods such as FTIR, NMR and MS. The antiproliferative activity of all synthesized compounds was evaluated against four cancer cell lines as well as the toxicity towards normal cells. Most of the synthesized compounds showed prominent activity against cancer cell lines HepG-2, HCT-116, MCF-7 and MDA-MB-231 with low toxicity towards normal cell BJ-1 compared to the starting 4-toluyl-1-toluyl phthalazine 1 as well as the reference drug doxorubicin. The IC50 values showed the prominence of all hybrids towards HepG-2 and HCT-116 cancer cell lines. The results showed that hybrid 6f was the best activity towards HepG-2, HCT-116, MCF-7 and MDA-MB-231 with IC50: 2.4, 6.8, 2.2, and 4.0 µM respectively.
Keywords
Heterocyclics; Phthalazine; Coumarin; Cancer Cell Lines
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