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

Author:
Barman, Surajit, Das, Gaurav, Mondal, Prasenjit, Pradhan, Krishnangsu, Jana, Batakrishna, Bhunia, Debmalya, Saha, Abhijit, Kar, Chirantan, Ghosh, Surajit
Source:
Chemical communications 2019 v.55 no.16 pp. 2356-2359
ISSN:
1364-548X
Subject:
antineoplastic activity, apoptosis, appendages, chemical compounds, microtubules, neoplasm cells, neoplasms, polymerization, propellers, tubulin
Abstract:
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.
Agid:
6312727