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
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-c...
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Nature Portfolio
2025-08-01
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| Series: | Scientific Reports |
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| Online Access: | https://doi.org/10.1038/s41598-025-13664-2 |
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| author | Anhar Abdel-Aziem Abdou O. Abdelhamid |
| author_facet | Anhar Abdel-Aziem Abdou O. Abdelhamid |
| author_sort | Anhar Abdel-Aziem |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-29c138a5eac24cc2a95df39a32f478c2 |
| institution | Kabale University |
| issn | 2045-2322 |
| language | English |
| publishDate | 2025-08-01 |
| publisher | Nature Portfolio |
| record_format | Article |
| series | Scientific Reports |
| spelling | doaj-art-29c138a5eac24cc2a95df39a32f478c22025-08-20T04:03:17ZengNature PortfolioScientific Reports2045-23222025-08-0115111010.1038/s41598-025-13664-2Utility 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 activityAnhar Abdel-Aziem0Abdou O. Abdelhamid1Department of Chemistry, Faculty of Science (Girls), Al-Azhar UniversityDepartment of Chemistry, Faculty of Science, Cairo UniversityAbstract 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.https://doi.org/10.1038/s41598-025-13664-2Coumarin1,3-thiazole1,3,4-thiadiazoleHydrazonoyl halidesCytotoxic activity |
| spellingShingle | Anhar Abdel-Aziem Abdou O. Abdelhamid 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 Scientific Reports Coumarin 1,3-thiazole 1,3,4-thiadiazole Hydrazonoyl halides Cytotoxic activity |
| title | 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 |
| title_full | 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 |
| title_fullStr | 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 |
| title_full_unstemmed | 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 |
| title_short | 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 |
| title_sort | 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 |
| topic | Coumarin 1,3-thiazole 1,3,4-thiadiazole Hydrazonoyl halides Cytotoxic activity |
| url | https://doi.org/10.1038/s41598-025-13664-2 |
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