Cryptophycin unit B analogues
Drug conjugates using toxic payloads are a promising approach for selectively combating cancer while sparing healthy tissue. The lack of highly cytotoxic and at the same time selective therapeutics against cancer is an ongoing challenge. Cryptophycins are a class of cyclic depsipeptides renowned for...
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| Format: | Article |
| Language: | English |
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Beilstein-Institut
2025-03-01
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| Series: | Beilstein Journal of Organic Chemistry |
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| Online Access: | https://doi.org/10.3762/bjoc.21.40 |
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| author | Thomas Schachtsiek Jona Voss Maren Hamsen Beate Neumann Hans-Georg Stammler Norbert Sewald |
| author_facet | Thomas Schachtsiek Jona Voss Maren Hamsen Beate Neumann Hans-Georg Stammler Norbert Sewald |
| author_sort | Thomas Schachtsiek |
| collection | DOAJ |
| description | Drug conjugates using toxic payloads are a promising approach for selectively combating cancer while sparing healthy tissue. The lack of highly cytotoxic and at the same time selective therapeutics against cancer is an ongoing challenge. Cryptophycins are a class of cyclic depsipeptides renowned for their high cytotoxicity in the picomolar range often combined with efficacy against multidrug-resistant tumour cell lines. However, cryptophycins failed as stand-alone drugs in cancer treatment, and their naturally occurring derivatives lack a covalent attachment handle. By making use of drug conjugates, toxic payloads such as cryptophycins can be selectively delivered to the target site. We present the synthesis of two conjugable cryptophycins with amino groups in unit B, representing potential payloads for drug conjugates particularly effective against multidrug-resistant cancers. |
| format | Article |
| id | doaj-art-50303f5bf92b44d6a8d693aea8d469e7 |
| institution | OA Journals |
| issn | 1860-5397 |
| language | English |
| publishDate | 2025-03-01 |
| publisher | Beilstein-Institut |
| record_format | Article |
| series | Beilstein Journal of Organic Chemistry |
| spelling | doaj-art-50303f5bf92b44d6a8d693aea8d469e72025-08-20T02:26:09ZengBeilstein-InstitutBeilstein Journal of Organic Chemistry1860-53972025-03-0121152653210.3762/bjoc.21.401860-5397-21-40Cryptophycin unit B analoguesThomas Schachtsiek0Jona Voss1Maren Hamsen2Beate Neumann3Hans-Georg Stammler4Norbert Sewald5Department of Chemistry, Organic and Bioorganic Chemistry, Bielefeld University, Universitätsstraße 25, 33615 Bielefeld, Germany Department of Chemistry, Organic and Bioorganic Chemistry, Bielefeld University, Universitätsstraße 25, 33615 Bielefeld, Germany Department of Chemistry, Organic and Bioorganic Chemistry, Bielefeld University, Universitätsstraße 25, 33615 Bielefeld, Germany Department of Chemistry, Inorganic and Structural Chemistry, Bielefeld University, Universitätsstraße 25, 33615 Bielefeld, Germany Department of Chemistry, Inorganic and Structural Chemistry, Bielefeld University, Universitätsstraße 25, 33615 Bielefeld, Germany Department of Chemistry, Organic and Bioorganic Chemistry, Bielefeld University, Universitätsstraße 25, 33615 Bielefeld, Germany Drug conjugates using toxic payloads are a promising approach for selectively combating cancer while sparing healthy tissue. The lack of highly cytotoxic and at the same time selective therapeutics against cancer is an ongoing challenge. Cryptophycins are a class of cyclic depsipeptides renowned for their high cytotoxicity in the picomolar range often combined with efficacy against multidrug-resistant tumour cell lines. However, cryptophycins failed as stand-alone drugs in cancer treatment, and their naturally occurring derivatives lack a covalent attachment handle. By making use of drug conjugates, toxic payloads such as cryptophycins can be selectively delivered to the target site. We present the synthesis of two conjugable cryptophycins with amino groups in unit B, representing potential payloads for drug conjugates particularly effective against multidrug-resistant cancers.https://doi.org/10.3762/bjoc.21.40cancer treatmentcryptophycinsdrug conjugatespayloadtargeted delivery |
| spellingShingle | Thomas Schachtsiek Jona Voss Maren Hamsen Beate Neumann Hans-Georg Stammler Norbert Sewald Cryptophycin unit B analogues Beilstein Journal of Organic Chemistry cancer treatment cryptophycins drug conjugates payload targeted delivery |
| title | Cryptophycin unit B analogues |
| title_full | Cryptophycin unit B analogues |
| title_fullStr | Cryptophycin unit B analogues |
| title_full_unstemmed | Cryptophycin unit B analogues |
| title_short | Cryptophycin unit B analogues |
| title_sort | cryptophycin unit b analogues |
| topic | cancer treatment cryptophycins drug conjugates payload targeted delivery |
| url | https://doi.org/10.3762/bjoc.21.40 |
| work_keys_str_mv | AT thomasschachtsiek cryptophycinunitbanalogues AT jonavoss cryptophycinunitbanalogues AT marenhamsen cryptophycinunitbanalogues AT beateneumann cryptophycinunitbanalogues AT hansgeorgstammler cryptophycinunitbanalogues AT norbertsewald cryptophycinunitbanalogues |