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

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Structure-activity relationships of analogues of thapsigargin modified at O-11 and O-12. / Nielsen, S F; Thastrup, Ole; Pedersen, R; Olsen, C E; Christensen, S B.

In: Journal of Medicinal Chemistry, Vol. 38, No. 2, 1995, p. 272-6.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Nielsen, SF, Thastrup, O, Pedersen, R, Olsen, CE & Christensen, SB 1995, 'Structure-activity relationships of analogues of thapsigargin modified at O-11 and O-12', Journal of Medicinal Chemistry, vol. 38, no. 2, pp. 272-6.

APA

Nielsen, S. F., Thastrup, O., Pedersen, R., Olsen, C. E., & Christensen, S. B. (1995). Structure-activity relationships of analogues of thapsigargin modified at O-11 and O-12. Journal of Medicinal Chemistry, 38(2), 272-6.

Vancouver

Nielsen SF, Thastrup O, Pedersen R, Olsen CE, Christensen SB. Structure-activity relationships of analogues of thapsigargin modified at O-11 and O-12. Journal of Medicinal Chemistry. 1995;38(2):272-6.

Author

Nielsen, S F ; Thastrup, Ole ; Pedersen, R ; Olsen, C E ; Christensen, S B. / Structure-activity relationships of analogues of thapsigargin modified at O-11 and O-12. In: Journal of Medicinal Chemistry. 1995 ; Vol. 38, No. 2. pp. 272-6.

Bibtex

@article{4e03444631f64f4f99ca5dcbf938475b,
title = "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.",
keywords = "Animals, Calcium-Transporting ATPases, Muscles, Rabbits, Structure-Activity Relationship, Terpenes, Thapsigargin",
author = "Nielsen, {S F} and Ole Thastrup and R Pedersen and Olsen, {C E} and Christensen, {S B}",
year = "1995",
language = "English",
volume = "38",
pages = "272--6",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "2",

}

RIS

TY - JOUR

T1 - Structure-activity relationships of analogues of thapsigargin modified at O-11 and O-12

AU - Nielsen, S F

AU - Thastrup, Ole

AU - Pedersen, R

AU - Olsen, C E

AU - Christensen, S B

PY - 1995

Y1 - 1995

N2 - 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.

AB - 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.

KW - Animals

KW - Calcium-Transporting ATPases

KW - Muscles

KW - Rabbits

KW - Structure-Activity Relationship

KW - Terpenes

KW - Thapsigargin

M3 - Journal article

C2 - 7830270

VL - 38

SP - 272

EP - 276

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 2

ER -

ID: 43349290