Abstract
Phenanthroindolizidine and phenanthroquinolizidine derivatives constitute a series of compounds that are being intensively studied as potential anticancer agents. Related natural products such as antofine and tylophorine alkaloids are well known for their high cytotoxic activity; however, their clinical application has been limited because of their side effects. In this review we report, in detail, on the main structural modifications applied to the phenanthroindolizidine and phenanthroquinolizidine skeletons, and we also describe their associated anticancer activities. New derivatives with promising antitumoral activities have emerged. Simplified analogues were prepared using rapid synthetic routes, and a certain number of these analogues displayed increased anticancer activity and selectivity towards tumor cell lines. It is hoped that a better understanding of the mechanisms of action associated with structure–activity relationships (SAR) will enable us to rationalize the development of new anticancer drugs.
Keywords: Alkaloids, anticancer, antofine, phenanthroindolizidine, phenanthroquinolizidine, structure–activity relationships, tylophorine.
Anti-Cancer Agents in Medicinal Chemistry
Title:Recent Advances in Phenanthroindolizidine and Phenanthroquinolizidine Derivatives with Anticancer Activities
Volume: 15 Issue: 9
Author(s): Maria de Fatima Pereira, Christophe Rochais and Patrick Dallemagne
Affiliation:
Keywords: Alkaloids, anticancer, antofine, phenanthroindolizidine, phenanthroquinolizidine, structure–activity relationships, tylophorine.
Abstract: Phenanthroindolizidine and phenanthroquinolizidine derivatives constitute a series of compounds that are being intensively studied as potential anticancer agents. Related natural products such as antofine and tylophorine alkaloids are well known for their high cytotoxic activity; however, their clinical application has been limited because of their side effects. In this review we report, in detail, on the main structural modifications applied to the phenanthroindolizidine and phenanthroquinolizidine skeletons, and we also describe their associated anticancer activities. New derivatives with promising antitumoral activities have emerged. Simplified analogues were prepared using rapid synthetic routes, and a certain number of these analogues displayed increased anticancer activity and selectivity towards tumor cell lines. It is hoped that a better understanding of the mechanisms of action associated with structure–activity relationships (SAR) will enable us to rationalize the development of new anticancer drugs.
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Fatima Pereira de Maria, Rochais Christophe and Dallemagne Patrick, Recent Advances in Phenanthroindolizidine and Phenanthroquinolizidine Derivatives with Anticancer Activities, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (9) . https://dx.doi.org/10.2174/1871520615666150520143600
DOI https://dx.doi.org/10.2174/1871520615666150520143600 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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