Anti-Cancerous Effect of 4,4'-Dihydroxychalcone ((2E,2'E)-3,3'-(1,4-Phenylene) Bis (1-(4-hydroxyphenyl) Prop-2-en-1-one)) on T47D Breast Cancer Cell Line

Abstract

Aims:The majority of human breast tumors are estrogen receptor α (ERα) positive. However, not all of the ERα+ breast cancers respond to anti-estrogens drugs for those women who do respond, initial positive responses can be of short duration. Thus, more effective drugs are needed to enhance the efficacy of anti-estrogens drugs or to be used separately in a period of time. In view of potential cytotoxicity associated with silybin as polyhydroxy compounds a synthetic 4-hydroxychalcones (bis-phenol) was considered to explore its anti-carcinogenic effects in comparison to silybin on ERα+ breast cancer cell line. Methodology: We have studied the inhibitory effect of 4,4'-dihydroxychalcone on the T47D breast cancer cell line by MTT test and the IC 50 s were estimated using Pharm PCS. Results: The 4,4'-dihydroxychalcone showed significant dose-and time-dependent cell growth inhibitory effects on T47D breast cancer cells. The IC 50 of 4,4'-dihydroxychalcone on T47D cells after 24 and 48 hours was 160.88+/-1 µM, 62.20+/-1 µM and for silybin was 373.42+/-1 µM,176.98+/-1 µM respectively.

Synthesis, biological evaluation, quantitative-SAR and docking studies of novel chalcone derivatives as antibacterial and antioxidant agents

“…The chalcones are precursors in the biosynthetic pathways of flavonoids, isoflavonoids, and aurone, which reportedly have wide-ranging pharmacological activities, such as antifungal (Zhao et al, 2007), antibacterial (Nielsen et al, 2005), antioxidant (Aichaoui et al, 2009), anticancer (Mahmoodi et al, 2014), antiprotozoal (Kiat et al, 2006), antiinflammatory (Seo et al, 2005), antimalarial (Awasthi et al, 2009), anti-HIV (Cheenpracha et al, 2006), anti-angiogenic (Varinska et al, 2012), cyclooxygenase inhibitory (Sharma, 2014) and tyrosine phosphatase 1B inhibitory activities (Sun et al, 2012). Chalcones and their α,β-dibromo derivatives (2,3-dibromo-1,3-diphenyl-2-propen-1-one) are used as intermediates for the syntheses of various heterocyclic compounds, such as flavones, flavonols, aziridines, coumarones, quinolines, pyrazoles and isooxazoles (Tökés et al, 1992;Wróblewski et al, 2000;Agrawal & Soni, 2007).…”