Synthesis and cytotoxic activity of certain benzothiazole derivatives against human MCF‐7 cancer cell line

Abstract

A new series of benzothiazole has been synthesized as cytotoxic agents. The new derivatives were tested for their cytotoxic activity toward the human breast cancer MCF-7 cell line against cisplatin as the reference drug. Many derivatives revealed good cytotoxic effect, whereas four of them, 4, 5c, 5d, and 6b, were more potent than cisplatin, with IC values being 8.64, 7.39, 7.56, and 5.15 μm compared to 13.33 μm of cisplatin. The four derivatives' cytotoxic activity was accompanied by regulating free radicals production, by increasing the activity of superoxide dismutase and depletion of intracellular reduced glutathione, catalase, and glutathione peroxidase activities, accordingly, the high production of hydrogen peroxide, nitric oxide, and other free radicals causing tumor cell death as monitored by reduction in the synthesis of protein and nucleic acids. Most of the tested compounds showed potent to moderate growth inhibitory activity; in particular, compound 6b exhibited the highest activity suggesting it is a lead compound in cytotoxic activity.

Synthesis of 2-Substituted Benzothiazole Derivatives and Their In Vitro Anticancer Effects and Antioxidant Activities Against Pancreatic Cancer Cells

“…Synthesized compounds have been a primary source from which various apoptosis-inducing agents are obtained. As reported by various scientific studies, synthesized compounds may be effective in cancer inhibition or therapy (23,37,38). These studies demonstrated that bioactive compounds cause apoptosis of tumor cells (20,39).…”

A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors

“…Benzothiazole is an important structure for drug development due to its favourable biological activity 120–122 . Benzothiazole compounds have biological activities such as antitumor 123 , anti-inflammatory 124 , antioxidation 125 , antibacterial 126 , and anti-diabetic 127 et al Benzothiazole-chalcones retain the basic structure of chalcones and replace the A or B rings with benzothiazoles to obtain chalcones with high antitumor activity and low toxicity.…”

Benzothiazole carbamates and amides as antiproliferative species

“…Benzothiazoles were investigated on several instances for their anti-cancer activity. 18,19,20,21,22,23,24,25,26 They were tested against selected number of cell lines, e.g., human cervical cancer, liver cancer, NSCL, prostate cancer, and human breast cancer exhibiting good to excellent antiproliferative activity with low toxicity. Former clinical candidate, Phortress (6), lysylamide prodrug of C(2) and C(6) substituted benzothiazole 5F203 (5), Figure 1)…”