Utility of 3-(2-oxo-2H-chromen-3-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde in the synthesis of novel 1,3,4-thiadiazoles or 1,3-thiazoles and study their cytotoxic activity

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Abstract One of the biggest causes of death around the world is cancer. Despite the development of a variety of chemotherapeutic drugs that stop excessive cell division, drug resistance remains a major obstacle to chemotherapy. It is consequently critical to develop and find new and effective anti-cancer agents in order to address the global threat. Owing to coumarins are a promising scaffold for anticancer agents, in this approach, we interested to synthesis new coumarins linked to either 1,3-thiazols or 1,3,4-thiadiazoles and examined their cytotoxic efficacy. Eleven of the newly prepared compounds were selected for the in vitro anticancer investigations against 60 human cancer cell lines at a single dose (10− 5M). Based on the results, we observed that compounds 3a, 3b, 6, 8a, b and 10b were the most active towards different cancer cell lines where the growth inhibition percent (GIP) was up to 96%. Moreover, compound 6 had lethality effect against melanoma MDA-MB-435 and renal cancer A498 with growth percent − 47.47 and − 6.20. Also, the lethal effects were seen with compound 10b where it exerted a value of − 27.79% toward melanoma MDA-MB-435.The highest GIP values 96.03% was recorded for compound 10a against melanoma MDA-MB-435 cancer cell line.

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