Structure-activity relationships of analogues of thapsigargin modified at O-11 and O-12
Research output: Contribution to journal › Journal article › Research › peer-review
A number of analogues of thapsigargin have been synthesized by alkylating or acylating O-11 and O-12 in the lactol obtained by reducing thapsigargicin. Introduction of alpha-disposed substituents decreased the Ca(2+)-ATPase inhibitory potency of the analogue, whereas the enzyme was more tolerant toward beta-disposed substituents, indicating that the alpha-face of the lactone ring is in close contact with the binding site when the inhibitor is bound to the enzyme.
Original language | English |
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Journal | Journal of Medicinal Chemistry |
Volume | 38 |
Issue number | 2 |
Pages (from-to) | 272-6 |
Number of pages | 5 |
ISSN | 0022-2623 |
Publication status | Published - 1995 |
- Animals, Calcium-Transporting ATPases, Muscles, Rabbits, Structure-Activity Relationship, Terpenes, Thapsigargin
Research areas
ID: 43349290