Anti-Cancer Agents in Medicinal Chemistry

(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Michelle Prudhomme  
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex


Recent Advances in Phenanthroindolizidine and Phenanthroquinolizidine Derivatives with Anticancer Activities

Author(s): Maria de Fatima Pereira, Christophe Rochais, Patrick Dallemagne.

Graphical 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.

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Article Details

Year: 2015
Page: [1080 - 1091]
Pages: 12
DOI: 10.2174/1871520615666150520143600
Price: $58