Synthesis and Anticancer Activity of 2’-hydroxy-2-bromo-4,5-dimetoxychalcone Against Breast Cancer (MCF-7) Cell Line

Abstract

Breast cancer is one of cancer causes of death in woman. Chemotherapy is one cancer treatment give toxic effects on normal cells. Alternative of cancer treatment by using flavonoid derivative have potent anticancer to reduce side effects of cancer. Chalcone is family of flavonoid that have biological activity. Chalcone derivatives have potential compound as anticancer agent. Chalcone with the presence halogen, metoxy group in ring B is know to inhibit cancer cells. The aims of this research were to synthesize chalcone derivate with bromo, methoxy, and hyroxy group in ring chalcone and to determine the anticancer activity of chalcone derivative. The chalcone derivative was synthesized from 2-hydroxyacetophenone with 2-bromo-4,5-dimethoxybenzaldehyde by Claisen-Schmidt reaction. In vitro cytotoxicity against breast cancer cell was tested by MTT assay method. The compound of 2’-hydroxy-2-bromo-4,5-dimethoxychalcone was yield in 78% as yellow solid. The IC50 of 2’-hydroxy-2-bromo-4,5-dimethoxychalcone was 42,19 µg/mL as a moderate activity to inhibiting breast cancer cell line. Cytotoxity of docorubicin againts breast cancer cell line more active than 2’-hydroxy-2-bromo-4,5-dimethoxychalcone with IC50 10,61 µg/mL. Doxorubicin as drug standar had better anticancer activity than 2’-hydroxy-2-bromo-4,5-dimethoxychalcone. Based on the IC50 value, the compound 2’-hydroxy-2-bromo-4,5-dimethoxychalcone has a moderate activity towards breast cancer cell lines. This study can recommend as candidate for anticancer againts breast cancer cell lines.

Finding a Novel Chalcone–Cinnamic Acid Chimeric Compound with Antiproliferative Activity against MCF-7 Cell Line Using a Free-Wilson Type Approach

“…A set of 207 molecules with cytotoxic activity against breast cancer line MCF-7 was selected from the literature [ 36 , 37 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 , 53 ]. Molecules express a variable range in their half-maximal inhibitory concentration (IC 50 ); see Table S1 .…”

Chalcones: Effective Agents for Fighting Cancer Across Multiple Cell Lines

“…Anwar and colleagues [29] synthesized a chalcone derivative by reacting 2‐hydroxyacetophenone with 2‐bromo‐4,5‐dimethoxybenzaldehyde, yielding (E)‐2’‐hydroxy‐2‐bromo‐4,5‐dimethoxychalcone 60 a . This novel chalcone derivative was evaluated for in vitro cytotoxicity against breast cancer cells using the MTT assay which resulted in an IC 50 value of 42.19 μg/mL, indicating moderate activity in inhibiting breast cancer cell growth.…”

Targeting autophagy with tamoxifen in breast cancer: From molecular mechanisms to targeted therapy

“…Breast cancer (BC) is one of the leading causes of mortality as well as the most prevalent type of cancer in women worldwide [1][2][3]. BC seems to be the cause of 18.2% of all cancer deaths, 16.2% of all female cancers, and 22.9% of invasive cancers [4]. Despite extensive research on the underlying processes of BC initiation and progression, patients suffering from BC are still facing high mortality rates [5,6].…”