Acetylenic antifolates as anticancer agents
Folates are crucial cofactors involved in the de novo generation of purine and deoxythymidine monophosphate, which are essential for DNA synthesis. Antifolates are structural analogues of folate derivatives that act as inhibitors of folate-dependent enzymes and constitute the oldest antimetabolite c...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
| Published: |
De Gruyter
2015-09-01
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| Series: | Pteridines |
| Subjects: | |
| Online Access: | https://doi.org/10.1515/pterid-2015-0006 |
| _version_ | 1819115191836606464 |
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| author | Önen Bayram Filiz Esra Sipahi Hande Akgün Hülya |
| author_facet | Önen Bayram Filiz Esra Sipahi Hande Akgün Hülya |
| author_sort | Önen Bayram Filiz Esra |
| collection | DOAJ |
| description | Folates are crucial cofactors involved in the de novo generation of purine and deoxythymidine monophosphate, which are essential for DNA synthesis. Antifolates are structural analogues of folate derivatives that act as inhibitors of folate-dependent enzymes and constitute the oldest antimetabolite class of anticancer agents. This review focuses on antifolates with remarkable anticancer activities that include a terminal alkyne function in their molecular structure. The properties of CB3717, a tremendous inhibitor of thymidylate synthase, are described, and the development of raltitrexed and pralatrexate, a dihydrofolate reductase inhibitor approved by the U.S. Food and Drug Administration (FDA) as the first drug for the treatment of relapsed and refractory peripheral T cell lymphoma are presented. |
| first_indexed | 2024-12-22T04:57:17Z |
| format | Article |
| id | doaj.art-72654ab5e2564d62912189197f5bcdd9 |
| institution | Directory Open Access Journal |
| issn | 0933-4807 2195-4720 |
| language | English |
| last_indexed | 2024-12-22T04:57:17Z |
| publishDate | 2015-09-01 |
| publisher | De Gruyter |
| record_format | Article |
| series | Pteridines |
| spelling | doaj.art-72654ab5e2564d62912189197f5bcdd92022-12-21T18:38:20ZengDe GruyterPteridines0933-48072195-47202015-09-01263859210.1515/pterid-2015-0006Acetylenic antifolates as anticancer agentsÖnen Bayram Filiz Esra0Sipahi Hande1Akgün Hülya2Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Yeditepe University, 26 Ağustos Yerleşimi, Kayışdağı, Istanbul, 34755, TurkeyFaculty of Pharmacy, Department of Toxicology, Yeditepe University, 26 Ağustos Yerleşimi, Kayışdağı, Istanbul, 34755, TurkeyFaculty of Pharmacy, Department of Pharmaceutical Chemistry, Yeditepe University, 26 Ağustos Yerleşimi, Kayışdağı, Istanbul, 34755, TurkeyFolates are crucial cofactors involved in the de novo generation of purine and deoxythymidine monophosphate, which are essential for DNA synthesis. Antifolates are structural analogues of folate derivatives that act as inhibitors of folate-dependent enzymes and constitute the oldest antimetabolite class of anticancer agents. This review focuses on antifolates with remarkable anticancer activities that include a terminal alkyne function in their molecular structure. The properties of CB3717, a tremendous inhibitor of thymidylate synthase, are described, and the development of raltitrexed and pralatrexate, a dihydrofolate reductase inhibitor approved by the U.S. Food and Drug Administration (FDA) as the first drug for the treatment of relapsed and refractory peripheral T cell lymphoma are presented.https://doi.org/10.1515/pterid-2015-0006antifolatecancercb3717pralatrexateraltitrexedterminal alkyne |
| spellingShingle | Önen Bayram Filiz Esra Sipahi Hande Akgün Hülya Acetylenic antifolates as anticancer agents Pteridines antifolate cancer cb3717 pralatrexate raltitrexed terminal alkyne |
| title | Acetylenic antifolates as anticancer agents |
| title_full | Acetylenic antifolates as anticancer agents |
| title_fullStr | Acetylenic antifolates as anticancer agents |
| title_full_unstemmed | Acetylenic antifolates as anticancer agents |
| title_short | Acetylenic antifolates as anticancer agents |
| title_sort | acetylenic antifolates as anticancer agents |
| topic | antifolate cancer cb3717 pralatrexate raltitrexed terminal alkyne |
| url | https://doi.org/10.1515/pterid-2015-0006 |
| work_keys_str_mv | AT onenbayramfilizesra acetylenicantifolatesasanticanceragents AT sipahihande acetylenicantifolatesasanticanceragents AT akgunhulya acetylenicantifolatesasanticanceragents |