Synthesis and structure elucidation of some novel thiophene and benzothiophene derivatives as cytotoxic agents
Attempting to produce cyclized systems with potential anti-proliferative activity, a series of novel thiophene and benzothiophene derivatives were designed and synthesized. The reactivity of the latter derivatives towards different chemical reagents was studied. Twenty-one compounds were synthesized...
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| Format: | Article |
| Language: | English |
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Sciendo
2016-03-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.1515/acph-2016-0005 |
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| author | Mohareb Rafat M. Abdallah Amira E. M. Helal Maher H. E. Shaloof Somiya M. H. |
| author_facet | Mohareb Rafat M. Abdallah Amira E. M. Helal Maher H. E. Shaloof Somiya M. H. |
| author_sort | Mohareb Rafat M. |
| collection | DOAJ |
| description | Attempting to produce cyclized systems with potential anti-proliferative activity, a series of novel thiophene and benzothiophene derivatives were designed and synthesized. The reactivity of the latter derivatives towards different chemical reagents was studied. Twenty-one compounds were synthesized and evaluated as anti-cancer agents. The results showed that ethyl 5-amino-3-(4-chlorostyryl)-4-cyanothiophene-2-carboxylate (5b), ethyl 5-amino-4-((4-methoxyphenyl)carbonyl)-3-methylhiophene-2-carboxylate (8c) and 5-3-(ethoxy-3-oxopropanamido)-3-methyl-4-(phenylcarbamoyl)thiophene-2-carboxylate (9) were the most active compounds towards three tumor cell lines – MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and SF-268 (CNS cancer) and a normal fibro-blast human cell line (WI-38) compared to the anti-proliferative effects of the reference control doxorubicin. |
| format | Article |
| id | doaj-art-c6fb6e97ec69479c970bde105db75ac3 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2016-03-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-c6fb6e97ec69479c970bde105db75ac32025-02-02T09:57:48ZengSciendoActa Pharmaceutica1846-95582016-03-01661536810.1515/acph-2016-0005acph-2016-0005Synthesis and structure elucidation of some novel thiophene and benzothiophene derivatives as cytotoxic agentsMohareb Rafat M.0Abdallah Amira E. M.1Helal Maher H. E.2Shaloof Somiya M. H.3 Department of Chemistry, Faculty of Science, Cairo University Giza, A. R. Egypt Department of Chemistry, Faculty of Science, Helwan University Ain Helwan, Cairo, A. R. Egypt Department of Chemistry, Faculty of Science, Helwan University Ain Helwan, Cairo, A. R. Egypt Department of Chemistry, Faculty of Science, Western Mountain University, Alzintan, LibyaAttempting to produce cyclized systems with potential anti-proliferative activity, a series of novel thiophene and benzothiophene derivatives were designed and synthesized. The reactivity of the latter derivatives towards different chemical reagents was studied. Twenty-one compounds were synthesized and evaluated as anti-cancer agents. The results showed that ethyl 5-amino-3-(4-chlorostyryl)-4-cyanothiophene-2-carboxylate (5b), ethyl 5-amino-4-((4-methoxyphenyl)carbonyl)-3-methylhiophene-2-carboxylate (8c) and 5-3-(ethoxy-3-oxopropanamido)-3-methyl-4-(phenylcarbamoyl)thiophene-2-carboxylate (9) were the most active compounds towards three tumor cell lines – MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and SF-268 (CNS cancer) and a normal fibro-blast human cell line (WI-38) compared to the anti-proliferative effects of the reference control doxorubicin.https://doi.org/10.1515/acph-2016-0005thiophenebenzothiophenecytotoxic agents |
| spellingShingle | Mohareb Rafat M. Abdallah Amira E. M. Helal Maher H. E. Shaloof Somiya M. H. Synthesis and structure elucidation of some novel thiophene and benzothiophene derivatives as cytotoxic agents Acta Pharmaceutica thiophene benzothiophene cytotoxic agents |
| title | Synthesis and structure elucidation of some novel thiophene and benzothiophene derivatives as cytotoxic agents |
| title_full | Synthesis and structure elucidation of some novel thiophene and benzothiophene derivatives as cytotoxic agents |
| title_fullStr | Synthesis and structure elucidation of some novel thiophene and benzothiophene derivatives as cytotoxic agents |
| title_full_unstemmed | Synthesis and structure elucidation of some novel thiophene and benzothiophene derivatives as cytotoxic agents |
| title_short | Synthesis and structure elucidation of some novel thiophene and benzothiophene derivatives as cytotoxic agents |
| title_sort | synthesis and structure elucidation of some novel thiophene and benzothiophene derivatives as cytotoxic agents |
| topic | thiophene benzothiophene cytotoxic agents |
| url | https://doi.org/10.1515/acph-2016-0005 |
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