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Focusing on accessing a fine-tuned family of \u03b1-acyloxyamide\u2013oxindole hybrids, we underline herein our latest insights regarding the use of this mild reaction approach to obtain promising anticancer agents. Cheap and commercially available isatin was used as starting material. The library of \u03b1-acyloxyamide\u2013oxindole hybrids was tested against six human solid-tumor cell lines; among them, non-small cell lung carcinoma, cervical and colon adenocarcinoma, and breast and pancreas cancer. The most potent compound displayed GI50 values in the range of 1.3\u201321 \u00b5M.<\/jats:p>","DOI":"10.3390\/molecules29235538","type":"journal-article","created":{"date-parts":[[2024,11,25]],"date-time":"2024-11-25T08:38:24Z","timestamp":1732523904000},"page":"5538","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Accessing Promising Passerini Adducts in Anticancer Drug Design"],"prefix":"10.3390","volume":"29","author":[{"ORCID":"https:\/\/orcid.org\/0009-0002-9310-2876","authenticated-orcid":false,"given":"Ana Margarida","family":"Janeiro","sequence":"first","affiliation":[{"name":"Faculty of Pharmacy, University of Lisbon, Av. Prof. Gama Pinto, 1649-003 Lisbon, Portugal"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9792-5194","authenticated-orcid":false,"given":"Aday","family":"Gonz\u00e1lez-Bakker","sequence":"additional","affiliation":[{"name":"BioLab, Instituto Universitario de Bio-Org\u00e1nica Antonio Gonz\u00e1lez (IUBO-AG), Universidad de La Laguna, P.O. Box 456, 38200 La Laguna, Spain"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6268-6552","authenticated-orcid":false,"given":"Jos\u00e9 M.","family":"Padr\u00f3n","sequence":"additional","affiliation":[{"name":"BioLab, Instituto Universitario de Bio-Org\u00e1nica Antonio Gonz\u00e1lez (IUBO-AG), Universidad de La Laguna, P.O. Box 456, 38200 La Laguna, Spain"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1697-7871","authenticated-orcid":false,"given":"Carolina S.","family":"Marques","sequence":"additional","affiliation":[{"name":"LAQV-REQUIMTE, Institute for Research and Advanced Studies, University of \u00c9vora, Rua Rom\u00e3o Ramalho, 59, 7000-641 \u00c9vora, Portugal"}]}],"member":"1968","published-online":{"date-parts":[[2024,11,23]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"376","DOI":"10.1021\/acsmedchemlett.3c00012","article-title":"Accelerating Drug Discovery: Synthesis of Complex Chemotypes via Multicomponent Reactions","volume":"14","author":"Buskes","year":"2023","journal-title":"ACS Med. Chem. Lett."},{"key":"ref_2","doi-asserted-by":"crossref","unstructured":"Cores, \u00c1., Clerigu\u00e9, J., Orocio-Rodr\u00edguez, E., and Men\u00e9ndez, J.C. (2022). Multicomponent Reactions for the Synthesis of Active Pharmaceutical Ingredients. 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