Tripodal molecular propellers perturb microtubule dynamics: indole acts as a blade and plays a crucial role in anticancer activity.

Surajit Barman,Gaurav Das,Prasenjit Mondal,Krishnangsu Pradhan,Batakrishna Jana,Debmalya Bhunia,Abhijit Saha,Chirantan Kar,Surajit Ghosh

CHEMICAL COMMUNICATIONS（2019）

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摘要

An indole-rich tripodal microtubule inhibitor is designed, which binds at the DCVJ site of tubulin and inhibits its polymerization. It causes apoptotic death of cancer cells without affecting normal cells and inhibits the growth of tumors. Finally, STD-NMR and TR-NOESY experiments reveal that the indole appendages play a crucial role in interacting with tubulin.

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