Synthesis, cytotoxic evaluation and structure activity relationship of pyrazole hybrid aurones on gastric cancer (AGS) cell lines
A series of pyrazole hybrid aurones have been synthesized and evaluated for their cytotoxic activity against AGS CRL-1739 cell line. The structures of these hybrid aurones were confirmed based on their IR, 1H NMR, 13C NMR, and HRMS data. The impact of these pyrazole hybrid aurones on cell viability...
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| Format: | Article |
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Elsevier
2022-01-01
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| Series: | Results in Chemistry |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211715622003095 |
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| author | Ekta Lathwal Sanjeev Kumar Pranab Kumar Sahoo Sushmita Ghosh Sutapa Mahata Vilas D. Nasare Suresh Kumar |
| author_facet | Ekta Lathwal Sanjeev Kumar Pranab Kumar Sahoo Sushmita Ghosh Sutapa Mahata Vilas D. Nasare Suresh Kumar |
| author_sort | Ekta Lathwal |
| collection | DOAJ |
| description | A series of pyrazole hybrid aurones have been synthesized and evaluated for their cytotoxic activity against AGS CRL-1739 cell line. The structures of these hybrid aurones were confirmed based on their IR, 1H NMR, 13C NMR, and HRMS data. The impact of these pyrazole hybrid aurones on cell viability and cytotoxic activity was studied on adenocarcinoma gastric cell line (AGS) using an in-vitro cell based MTT assay. Hybrid compounds 5e, 5f, 5i and 6g with IC50 25, 28.3, 27 and 25.1 (µM), respectively, were seen to have reduced cell viability and thus showed better cytotoxic activity in comparison to the standard chemotherapeutic drug agent Oxaliplatin (IC50 = 29.8 µM) and Leucovorin (IC50 = 30.8 µM),. Therefore, this study demonstrated that these compounds can be effective and potential anticancer agents with reliable efficacy. Analyzing this molecular library of thirty-five structurally related compounds, a concrete structure–activity relationship has been obtained. Compounds with 4-methylphenyl group at the 1st position of linked pyrazole moiety showed better cytotoxicity compared to phenyl and 4-nitrophenyl group with few exceptions. |
| first_indexed | 2024-04-13T05:53:24Z |
| format | Article |
| id | doaj.art-c8866692295249808d68f14e39234ea8 |
| institution | Directory Open Access Journal |
| issn | 2211-7156 |
| language | English |
| last_indexed | 2024-04-13T05:53:24Z |
| publishDate | 2022-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Results in Chemistry |
| spelling | doaj.art-c8866692295249808d68f14e39234ea82022-12-22T02:59:41ZengElsevierResults in Chemistry2211-71562022-01-014100590Synthesis, cytotoxic evaluation and structure activity relationship of pyrazole hybrid aurones on gastric cancer (AGS) cell linesEkta Lathwal0Sanjeev Kumar1Pranab Kumar Sahoo2Sushmita Ghosh3Sutapa Mahata4Vilas D. Nasare5Suresh Kumar6Department of Chemistry, Kurukshetra University, Kurukshetra 136119, Haryana, India; Govt. College, Tigaon, Faridabad 121101, Haryana, IndiaDepartment of Chemistry, Kurukshetra University, Kurukshetra 136119, Haryana, India; PGT Chemistry, Kendriya Vidyalaya Kokrajhar, Assam 783370, IndiaDepartment of Pathology and Cancer Screening, Chittaranjan National Cancer Institute, 37, S.P. Mukherjee Road, Kolkata, IndiaDepartment of Pathology and Cancer Screening, Chittaranjan National Cancer Institute, 37, S.P. Mukherjee Road, Kolkata, IndiaDepartment of Pathology and Cancer Screening, Chittaranjan National Cancer Institute, 37, S.P. Mukherjee Road, Kolkata, IndiaDepartment of Pathology and Cancer Screening, Chittaranjan National Cancer Institute, 37, S.P. Mukherjee Road, Kolkata, IndiaDepartment of Chemistry, Kurukshetra University, Kurukshetra 136119, Haryana, India; Corresponding author.A series of pyrazole hybrid aurones have been synthesized and evaluated for their cytotoxic activity against AGS CRL-1739 cell line. The structures of these hybrid aurones were confirmed based on their IR, 1H NMR, 13C NMR, and HRMS data. The impact of these pyrazole hybrid aurones on cell viability and cytotoxic activity was studied on adenocarcinoma gastric cell line (AGS) using an in-vitro cell based MTT assay. Hybrid compounds 5e, 5f, 5i and 6g with IC50 25, 28.3, 27 and 25.1 (µM), respectively, were seen to have reduced cell viability and thus showed better cytotoxic activity in comparison to the standard chemotherapeutic drug agent Oxaliplatin (IC50 = 29.8 µM) and Leucovorin (IC50 = 30.8 µM),. Therefore, this study demonstrated that these compounds can be effective and potential anticancer agents with reliable efficacy. Analyzing this molecular library of thirty-five structurally related compounds, a concrete structure–activity relationship has been obtained. Compounds with 4-methylphenyl group at the 1st position of linked pyrazole moiety showed better cytotoxicity compared to phenyl and 4-nitrophenyl group with few exceptions.http://www.sciencedirect.com/science/article/pii/S2211715622003095AuronePyrazoleSynthesisAGS cancer cell line |
| spellingShingle | Ekta Lathwal Sanjeev Kumar Pranab Kumar Sahoo Sushmita Ghosh Sutapa Mahata Vilas D. Nasare Suresh Kumar Synthesis, cytotoxic evaluation and structure activity relationship of pyrazole hybrid aurones on gastric cancer (AGS) cell lines Results in Chemistry Aurone Pyrazole Synthesis AGS cancer cell line |
| title | Synthesis, cytotoxic evaluation and structure activity relationship of pyrazole hybrid aurones on gastric cancer (AGS) cell lines |
| title_full | Synthesis, cytotoxic evaluation and structure activity relationship of pyrazole hybrid aurones on gastric cancer (AGS) cell lines |
| title_fullStr | Synthesis, cytotoxic evaluation and structure activity relationship of pyrazole hybrid aurones on gastric cancer (AGS) cell lines |
| title_full_unstemmed | Synthesis, cytotoxic evaluation and structure activity relationship of pyrazole hybrid aurones on gastric cancer (AGS) cell lines |
| title_short | Synthesis, cytotoxic evaluation and structure activity relationship of pyrazole hybrid aurones on gastric cancer (AGS) cell lines |
| title_sort | synthesis cytotoxic evaluation and structure activity relationship of pyrazole hybrid aurones on gastric cancer ags cell lines |
| topic | Aurone Pyrazole Synthesis AGS cancer cell line |
| url | http://www.sciencedirect.com/science/article/pii/S2211715622003095 |
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