Seven novel pyrazole derivatives (4a-g) and four novel starting compounds incorporating substituted pyridine moieties were synthesized successfully. Cell viability assay for the tested compounds was performed, and the inhibitory concentrationlogarithmic 50 (LogIC 50 ) values of the compounds were calculated after a 24-h treatment. Four of the examined compounds (3d, 3g, 4f, and 4g) showed comparable cytotoxic activity against CaCo-2 compared to the standard drug docetaxel at 0.1 and 1 μM concentrations.Although the LogIC 50 of docetaxel was −0.678 μM for CaCo-2 cells at 24 h, the LogIC 50 values of compounds were −0.794, −0.567, −0.657, and −0.498 μM, respectively. Five of the compounds (2d, 2g, 3d, 3g, and 4e) showed comparable cytotoxic activity against MCF-7 at 0.1 μM concentration compared to docetaxel (p < 0.05). Docking studies revealed the compounds have a good affinity to the active site of the human topoisomerase II β enzyme. The antioxidant capacities of all compounds were determined using both 1,1-diphenyl-2-picrylhydrazyl and metal chelation methods. Although the compounds did not show significant antioxidant activity, relatively effective are compounds 3c, 3d, and 3g, which are hydrazine derivatives with approximately 50% antioxidant activity of standard antioxidants at concentrations of 62.5 and 125 μg/ml.
Six new monopeptides, seven new dipeptides, and two deprotected monopeptide dihydroquinolinone conjugates were prepared by the benzothiazole-mediated method and their structures were confirmed by nuclear magnetic resonance, mass, infrared spectroscopy, and elemental analysis methods. The human carbonic anhydrase (hCA) I and hCA II enzyme inhibition activities of the compounds were determined using the stopped-flow instrument.The synthesized peptide-dihydroquinolinone conjugates 2, 3, 6, 10, 13, and 15 showed inhibition against the hCA II enzyme in the range of 15.7-65.7 µM. However, none of the compounds showed inhibition of hCA I at a concentration of 100 µM. The antioxidant activities of the compounds were also examined using the DPPH (2,2diphenyl-1-picrylhydrazyl) radical scavenging method at concentrations of 12.5-125 µg/ml, but when compared with the standard antioxidant compounds αtocopherol and butylated hydroxyanisole (BHA), weak antioxidant activities were detected. The cytotoxic effects of four compounds against the A549 and BEAS-2B cell lines were also investigated. Among the compounds studied, compound 7 was found to be most effective, with the IC 50 values on the A549 cells for 48 and 72 h being 26.87 and 9.979 µg/ml, respectively, and the IC 50 values on the BEAS-2B cells being >100 µg/ml. None of the tested compounds showed antimicrobial activity in the concentration range (800-1.56 µg/ml) studied.
In this study, 10 new indole-dipeptide conjugates were synthesized, and their anticancer activity was determined against on A2780 (ovarian cancer cell line) and MCF-7 (breast cancer cell line) cells. Among compounds, 5 and 10 showed better activity against A2780 cell lines than the standard drug docatexel at 0.1 and 1 μM concentrations, while only compound 5 showed better activity than docatexel, the MCF-7 cell line at 0.1 and 1 μM concentrations. The antioxidant potencies of the compounds were low in both the DPPH and iron reducing power methods tested when compared to standard antioxidants used in this work. | INTRODUCTIONAccording to the 2020 report of the World Health Organization (WHO), the most common cancer cases worldwide are breast cancer with 47.8% and ovarian cancer with 6.6%. In 2020, there were 2.3 million women diagnosed with breast cancer and 685,000 deaths globally. According to WHO, all cancer-related deaths were reported as 10 million in 2020 [1,2]. Cancer R&D investment has the largest share in other pharmaceutical R&D expenditures, and this value is estimated to reach 82 billion by 2026. Thanks to these R&D investments, it is estimated that 152 new FDA-approved anticancer drugs and 311 billion drugs will be sold in 2026 [3]. Despite this high-mortality rate and spending on anticancer treatment around the
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