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Owing to their ability to modulate key oncogenic signaling pathways, quinoline\u2010based scaffolds have gained considerable attention in anticancer drug discovery. However, conventional synthetic routes for quinoline derivatives often suffer from prolonged reaction times, harsh conditions, low atom economy, and environmental concerns. In this context, green and sustainable synthetic methodologies have emerged as viable alternatives to address these limitations. Among them, microwave\u2010 and ultrasound\u2010assisted synthesis (UAS) have proven to be highly efficient non\u2010classical activation techniques, offering rapid reaction rates, improved yields, enhanced selectivity, and reduced energy consumption. This review provides a comprehensive overview of recent advances in the microwave\u2010 and UAS of quinoline derivatives with anticancer potential. Emphasis is placed on reaction efficiency, eco\u2010friendly reaction conditions, and the biological relevance of the synthesized compounds, including their cytotoxicity profiles, enzyme inhibition activities, and apoptosis\u2010inducing mechanisms. Collectively, this compilation highlights the integration of green chemistry principles into medicinal chemistry workflows and underscores the potential of sustainable synthetic strategies for the development of potent and selective quinoline\u2010based anticancer agents.<\/jats:p>","DOI":"10.1002\/cbdv.71675","type":"journal-article","created":{"date-parts":[[2026,9,21]],"date-time":"2026-09-21T06:27:59Z","timestamp":1789972079000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Recent Advances in Microwave and Ultrasound Assisted Synthesis of Quinoline Derivatives as Anticancer Agents"],"prefix":"10.1002","volume":"23","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-2763-5757","authenticated-orcid":false,"given":"Rohit","family":"Pal","sequence":"first","affiliation":[{"name":"Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry Acharya &amp; BM Reddy College of Pharmacy  Bengaluru Karnataka India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gurubasavaraja Swamy Purawarga","family":"Matada","sequence":"additional","affiliation":[{"name":"Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry Acharya &amp; BM Reddy College of Pharmacy  Bengaluru Karnataka India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ghanshyam","family":"Teli","sequence":"additional","affiliation":[{"name":"School of Pharmacy Sangam University, Atoon  Bhilwara Rajasthan India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Manjushree","family":"B V","sequence":"additional","affiliation":[{"name":"Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry Acharya &amp; BM Reddy College of Pharmacy  Bengaluru Karnataka India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Vipin K.","family":"Pandey","sequence":"additional","affiliation":[{"name":"School of Pharmacy Sangam University, Atoon  Bhilwara Rajasthan India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shourya","family":"Pratap","sequence":"additional","affiliation":[{"name":"Arni School of Pharmacy Arni University  Tanda Himachal Pradesh India"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2026,9,20]]},"reference":[{"key":"e_1_2_11_2_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules21040492"},{"key":"e_1_2_11_3_1","volume-title":"Advanced Medicinal Chemistry","author":"Metri D. 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