Determination of anti-carcinogenic and anti-inflammatory activities of new generation benzothiophene derivatives inclusive of aldehyde functional group

Cancer is the uncontrolled proliferation of cells with DNA damage, that is, mutations, that have lost their physiological properties. There are many types of cancer, and despite many advances to date, resistance to treatment remains a current threat, leading to recurrence in many cases. It is known that thiophene-containing heterocyclic compounds target cancer-specific proteins, causing inhibition or activation of important signaling pathways. The sulfur heterocyclic family includes highly stable aromatic compounds that exhibit physicochemical properties. In recent years, with the studies carried out, heterocyclic compounds containing thiophene have great importance in the field of health due to their properties such as anticancer, antioxidant, antifungal, antibacterial and antiparasitic. Benzothiophene is among the best-known heteroaromatic structures, and its derivatives have become popular in cancer research due to their emerging pharmacological properties. Raloxifene and Tamoxifen are examples of benzothiophene derivatives used as drugs for therapeutic purposes. In this thesis study, new generation Benzothiophene derivatives containing Aldehyde functional group have cytotoxic, anti- and anti-toxic effects on Human Lung Cancer (A549), Human Cervix Cancer (HeLa), Human Colorectal Cancer (Caco-2), Human Breast Cancer (MDA-MB-231) cell lines. Carcinogenic and anti-inflammatory activities have been determined. While the synthesized Q18, Q19, Q20 compounds had a significant apoptotic effect on Caco-2, MDA, HeLa cell lines, it was determined that the Q21 compound had no cytotoxic effect against the cells used in the study. In the results obtained by quantifying mRNA levels with the Real-Time PCR method, it was determined that compounds Q18, Q19, Q20 induced apoptosis-related genes (BAX, BCL-2, CASP3, CASP8, CASP9) in HeLa and MDA cell lines. In addition, all of the compounds used were found to highly inhibit the expression levels of pro-inflammatory genes (COX-2, iNOS, IL-6, TNF-ɑ). As a result of the study, it was revealed that the mentioned benzothiophene derivatives caused apoptosis induction and had cytotoxic effects. As a result, it has been shown that the benzothiophene derivatives synthesized for this thesis study may have the potential to be used in cancer treatment and as anti-inflammatory.