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Isocombretastatins a versus combretastatins a: the forgotten isoCA-4 isomer as a highly promising cytotoxic and antitubulin agent.

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Messaoudi, Samir | Tréguier, Bret | Hamze, Abdallah | Provot, Olivier | Peyrat, Jean-François | de Losada, Jordi Rodrigo | Liu, Jian-Miao | Bignon, Jérôme | Wdzieczak-Bakala, Joanna | Thoret, Sylviane | Dubois, Joëlle | Brion, Jean-Daniel | Alami, Mouâd

Edité par CCSD ; American Chemical Society -

International audience. Herein is reported a convergent synthesis of isocombretastatins A, a novel class of potent antitubulin agents. These compounds having a 1,1-diarylethylene scaffold constitute the simplest isomers of natural Z-combretastatins A that are easy to synthesize without need to control the Z-olefin geometry. The discovery of isoCA-4 with biological activities comparable to that of CA-4 represents a major progress in this field.

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