Accessing Promising Passerini Adducts in Anticancer Drug Design
The 3-component Passerini reaction (3CPR), discovered little more than 100 years ago, has been demonstrated in the last few decades to be a valuable tool for accessing structural diversity and complexity, essential topics to consider in drug discovery programs. Focusing on accessing a fine-tuned fam...
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| Format: | Article |
| Language: | English |
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MDPI AG
2024-11-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/29/23/5538 |
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| author | Ana Margarida Janeiro Aday González-Bakker José M. Padrón Carolina S. Marques |
| author_facet | Ana Margarida Janeiro Aday González-Bakker José M. Padrón Carolina S. Marques |
| author_sort | Ana Margarida Janeiro |
| collection | DOAJ |
| description | The 3-component Passerini reaction (3CPR), discovered little more than 100 years ago, has been demonstrated in the last few decades to be a valuable tool for accessing structural diversity and complexity, essential topics to consider in drug discovery programs. Focusing on accessing a fine-tuned family of α-acyloxyamide–oxindole 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 α-acyloxyamide–oxindole 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 GI<sub>50</sub> values in the range of 1.3–21 µM. |
| format | Article |
| id | doaj-art-b8211c65bcd04eaf9b0d4d7b86b4fbf3 |
| institution | Kabale University |
| issn | 1420-3049 |
| language | English |
| publishDate | 2024-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj-art-b8211c65bcd04eaf9b0d4d7b86b4fbf32024-12-13T16:28:13ZengMDPI AGMolecules1420-30492024-11-012923553810.3390/molecules29235538Accessing Promising Passerini Adducts in Anticancer Drug DesignAna Margarida Janeiro0Aday González-Bakker1José M. Padrón2Carolina S. Marques3Faculty of Pharmacy, University of Lisbon, Av. Prof. Gama Pinto, 1649-003 Lisbon, PortugalBioLab, Instituto Universitario de Bio-Orgánica Antonio González (IUBO-AG), Universidad de La Laguna, P.O. Box 456, 38200 La Laguna, SpainBioLab, Instituto Universitario de Bio-Orgánica Antonio González (IUBO-AG), Universidad de La Laguna, P.O. Box 456, 38200 La Laguna, SpainLAQV-REQUIMTE, Institute for Research and Advanced Studies, University of Évora, Rua Romão Ramalho, 59, 7000-641 Évora, PortugalThe 3-component Passerini reaction (3CPR), discovered little more than 100 years ago, has been demonstrated in the last few decades to be a valuable tool for accessing structural diversity and complexity, essential topics to consider in drug discovery programs. Focusing on accessing a fine-tuned family of α-acyloxyamide–oxindole 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 α-acyloxyamide–oxindole 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 GI<sub>50</sub> values in the range of 1.3–21 µM.https://www.mdpi.com/1420-3049/29/23/5538Passerini-3CoxindoleisatincancerGI<sub>50</sub>drug design |
| spellingShingle | Ana Margarida Janeiro Aday González-Bakker José M. Padrón Carolina S. Marques Accessing Promising Passerini Adducts in Anticancer Drug Design Molecules Passerini-3C oxindole isatin cancer GI<sub>50</sub> drug design |
| title | Accessing Promising Passerini Adducts in Anticancer Drug Design |
| title_full | Accessing Promising Passerini Adducts in Anticancer Drug Design |
| title_fullStr | Accessing Promising Passerini Adducts in Anticancer Drug Design |
| title_full_unstemmed | Accessing Promising Passerini Adducts in Anticancer Drug Design |
| title_short | Accessing Promising Passerini Adducts in Anticancer Drug Design |
| title_sort | accessing promising passerini adducts in anticancer drug design |
| topic | Passerini-3C oxindole isatin cancer GI<sub>50</sub> drug design |
| url | https://www.mdpi.com/1420-3049/29/23/5538 |
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