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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis of Chalcone Derivatives and Their Effects on Proliferation and Tubulin Dynamics Instability of HT-29 Cells

Author(s): Yasmin Tajuddin, Zaliha Harun, Ahmad Rohi Ghazali, Juriyati Jalil and Malina Jasamai

Volume 13, Issue 7, 2016

Page: [662 - 667] Pages: 6

DOI: 10.2174/157018081307160630182605

Price: $65


Chalcone derivatives are known for their numerous biological activities which include the interference of microtubule dynamics instability and are good candidates as an antimitotic agent that can be beneficial in the treatment of cancer. In the work described here, two series of chalcone derivatives including two newly synthesised derivatives were assessed for their antiproliferative activity and inhibition and promoting effects of tubulin polymerization. Antiproliferative activity was evaluated using the Microculture Tetrazolium (MTT) Assay while disruption of the mictotubule dynamics instability was investigated by the Tubulin Polymerization Assay. Both assays were carried out using human colon adenocarcinoma grade II (HT-29) cells. Compounds in series 5 showed strong inhibitory activity on the growth of HT-29 cells with IC50 ranging from 19.26 to 36.95 µM. Two of the chalcone derivatives, compound 5a and 5c were found to be active as an inhibitor and a promoter towards the microtubule dynamics respectively. Compounds with a dimethoxy benzene group on Ring B showed inhibitory effect of the HT-29 cells growth while furan on Ring A showed inhibitory effect on tubulin polymerization. These compounds are worthy to be investigated further as potential antimitotic agents.

Keywords: Chalcone, antiproliferative, inhibitor, promoter, tubulin, polymerization.

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