Synthesis of Flavokawain B, Curcumin, and Damnacanthal derivatives and their Potential Cytotoxic effect on the Breast Cancer Cell Lines, MCF-7, and MDA-MB231 | [Abstract Book on Global Science Technology and Management Conference • 2023]

Author(s):

1. Muhammad Nadeem Akhtar: Département of Chemistry, Ghazi University, Dera Ghazi Khan 32200, Pakistan; Faculty of Industrial Sciences & Technology, Universiti Malaysia Pahang, Lebuhraya Tun Razak 26300, Kuantan Pahang, Malaysia

2. Swee Keong Yeap: Institute of Bioscience, Universiti Putra Malaysia, UPM Serdang 43400, Selangor Darul Ehsan, Malaysia

3. Noorjahan Banu Alitheen: Faculty of Biotechnology and Bimolecular Sciences, Universiti Putra Malaysia, Serdang, Selangor Darul Ehsan, Malaysia

4. Seema Zareen: Faculty of Industrial Sciences & Technology, Universiti Malaysia Pahang, Lebuhraya Tun Razak 26300, Kuantan Pahang, Malaysia

Abstract:

Flavokawain B, a natural chalcone extracted from the roots of Piper methysticum and has been proven to be a potent cytotoxic compound. By using the partial structure of flavokawain B (FKB), about 23 analogs have been synthesized. Among them, compounds 8, 13, and 23 were 29 found to be new FKB derivatives. All compounds have been evaluated for their cytotoxic properties by using an MTT cell viability assay against two breast cancer cell lines MCF-7 and MDA-MB-231 and 31 thus establishing the structure-activity relationship. FKB derivatives, 16 (IC50 = 6.50±0.40 and 32 4.12±0.20), 15 (IC50 = 5.50±0.35 and 6.50±1.40) and 13 (IC50 = 7.12±0.80 and 4.04±0.30) exhibited 33 potential cytotoxic effects on MCF-7 and MDA-MB-231 cell lines. However, methoxy group meta substituted at positions 3 & 4 in compound 2 (IC50 = 8.90±0.60 and 6.80±0.35) and 22 (IC50 = 8.80±0.35 35 and 14.16±1.10) exhibited good cytotoxicity. The lead compound FKB showed potential cytotoxicity (IC50 = 7.70±0.30 and 5.90±0.30) against two proposed breast cancer cell lines. These findings could help to improve the future drug discovery process against breast cancer. Docking studies of active compounds 4 revealed the stable interactions within the active site of Janus Kinase. The structures of all compounds were determined by 1H-NMR, EI-MS, IR, and UV and X-ray crystallographic and spectroscopies techniques. The latest finding as a flavokawain B potential cytotoxic agent will be presented.

Page(s): 53-53

DOI: DOI not available

Published: Journal: Abstract Book on Global Science Technology and Management Conference, Volume: 0, Issue: 0, Year: 2023

Keywords:

Curcumin , Flavokawain B , Damnacanthal derivatives , Breast Cancer Cell Lines

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