Synthesis of chalcone derivatives and their effects on proliferation and tubulin dynamics instability of HT-29 Cells

Yasmin Tajuddin, Zaliha Harun, Ahmad Rohi Ghazali, Juriyati Jalil, Malina Jasamai

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Abstract

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 36.95M. 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.

Original languageEnglish
Pages (from-to)662-667
Number of pages6
JournalLetters in Drug Design and Discovery
Volume13
Issue number7
Publication statusPublished - 1 Aug 2016

Fingerprint

Chalcone
HT29 Cells
Tubulin
Polymerization
Antimitotic Agents
Microtubules
Growth
Benzene
Inhibitory Concentration 50
Colon
Adenocarcinoma
Neoplasms

Keywords

  • Antiproliferative
  • Chalcone
  • Inhibitor
  • Polymerization
  • Promoter
  • Tubulin

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Molecular Medicine

Cite this

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AU - Ghazali, Ahmad Rohi

AU - Jalil, Juriyati

AU - Jasamai, Malina

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