{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,2]],"date-time":"2026-10-02T22:48:12Z","timestamp":1790981292350,"version":"4.1.0"},"reference-count":55,"publisher":"MDPI AG","issue":"19","license":[{"start":{"date-parts":[[2020,10,6]],"date-time":"2020-10-06T00:00:00Z","timestamp":1601942400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Based on reported results for the potential medicinal impact of phenothiazine core, as well as the chalcone skeleton that is widely present in many natural products, together with their reported bioactivities, the present work was aimed at combining both moieties in one molecular skeleton and to synthesize and characterize a novel series of chalone-based phenothiazine derivatives. For this purpose, 2-acetylphenothiazine was N-alkylated, followed by the Claisen-Schmidt reaction to produce the chalcones with good yield. Antioxidant activity, as evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging, was assessed to determine if their antioxidant potential was comparable with ascorbic acid, and attributable to the phenothiazine core. Screening anticancer activities of the synthesized chalone-based phenothiazine derivatives against human breast cancer cell line MCF-7 cells, and human hepatocellular carcinoma HepG-2 cells, compared with standard drugs cisplatin and doxorubicin, was evaluated. The results revealed that compounds 4a, 4b, 4d, 4h, 4j, 4k, 4m, 4o, and 4p were good against human hepatocellular carcinoma HepG-2 cells, and among these compounds 4b and 4k were the most effective compounds, with IC50 values of 7.14 \u03bcg\/mL and 7.6 1 \u03bcg\/mL, respectively. On the other hand, compounds 4a, 4b, 4k, and 4m were good against human breast cancer cell line MCF-7 cells and, among these compounds, 4k and 4b were the most effective compounds, with IC50 values of 12 \u03bcg\/mL and 13. 8 \u03bcg\/mL, respectively. The overall results suggest that these compounds could, potentially, be further modified for the formation of more potent antioxidant and anticancer agents.<\/jats:p>","DOI":"10.3390\/molecules25194566","type":"journal-article","created":{"date-parts":[[2020,10,7]],"date-time":"2020-10-07T09:12:58Z","timestamp":1602061978000},"page":"4566","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":114,"title":["Synthesis of Novel Chalcone-Based Phenothiazine Derivatives as Antioxidant and Anticancer Agents"],"prefix":"10.3390","volume":"25","author":[{"given":"Nourah A.","family":"Al Zahrani","sequence":"first","affiliation":[{"name":"Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia"},{"name":"Chemistry Department, Faculty of Science, University of Jeddah, Jeddah 21959, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7744-529X","authenticated-orcid":false,"given":"Reda M.","family":"El-Shishtawy","sequence":"additional","affiliation":[{"name":"Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia"},{"name":"Dyeing, Printing and Textile Auxiliaries Department, Textile Research Division, National Research Centre, Dokki, Cairo 12611, Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0862-7628","authenticated-orcid":false,"given":"Mahmoud M.","family":"Elaasser","sequence":"additional","affiliation":[{"name":"The Regional Center for Mycology and Biotechnology, Al-Azhar University, Cairo 11759, Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Abdullah M.","family":"Asiri","sequence":"additional","affiliation":[{"name":"Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia"},{"name":"Center of Excellence for Advanced Materials Research, King Abdulaziz University, Jeddah 21589, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2020,10,6]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","unstructured":"Halliwell, B., and Gutteridge, J.M.C. 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