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Structure-activity relationships of analogues of thapsigargin modified at O-11 and O-12.

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Nielsen SF,Thastrup O,Pedersen R,Olsen CE,Christensen SB

doi

10.1021/jm00002a009

subject

Has Abstract

pub_date

1995-01-20 00:00:00

pages

272-6

issue

2

eissn

0022-2623

issn

1520-4804

journal_volume

38

pub_type

杂志文章

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