Details
| Original language | English |
|---|---|
| Pages (from-to) | 6550-6560 |
| Number of pages | 11 |
| Journal | Journal of the American Chemical Society |
| Volume | 138 |
| Issue number | 20 |
| Publication status | Published - 25 May 2016 |
| Externally published | Yes |
Abstract
A series of δ 12-prostaglandin J 3 (δ 12-PGJ 3) analogues and derivatives were synthesized employing an array of synthetic strategies developed specifically to render them readily available for biological investigations. The synthesized compounds were evaluated for their cytotoxicity against a number of cancer cell lines, revealing nanomolar potencies for a number of them against certain cancer cell lines. Four analogues (2, 11, 21, and 27) demonstrated inhibition of nuclear export through a covalent addition at Cys528 of the export receptor Crm1. One of these compounds (i.e., 11) is currently under evaluation as a potential drug candidate for the treatment of certain types of cancer. These studies culminated in useful and path-pointing structure-activity relationships (SARs) that provide guidance for further improvements in the biological/pharmacological profiles of compounds within this class.
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In: Journal of the American Chemical Society, Vol. 138, No. 20, 25.05.2016, p. 6550-6560.
Research output: Contribution to journal › Article › Research › peer review
}
TY - JOUR
T1 - Synthesis and Biological Investigation of Delta(12)-Prostaglandin J3 (Delta(12)-PGJ(3)) Analogues and Related Compounds
AU - Nicolaou, K. C.
AU - Pulukuri, Kiran Kumar
AU - Rigol, Stephan
AU - Heretsch, Philipp
AU - Yu, Ruocheng
AU - Grove, Charles I.
AU - Hale, Christopher R. H.
AU - ElMarrouni, Abdelatif
AU - Fetz, Verena
AU - Broenstrup, Mark
AU - Aujay, Monette
AU - Sandoval, Joseph
AU - Gavrilyuk, Julia
N1 - Publisher Copyright: © 2016 American Chemical Society.
PY - 2016/5/25
Y1 - 2016/5/25
N2 - A series of δ 12-prostaglandin J 3 (δ 12-PGJ 3) analogues and derivatives were synthesized employing an array of synthetic strategies developed specifically to render them readily available for biological investigations. The synthesized compounds were evaluated for their cytotoxicity against a number of cancer cell lines, revealing nanomolar potencies for a number of them against certain cancer cell lines. Four analogues (2, 11, 21, and 27) demonstrated inhibition of nuclear export through a covalent addition at Cys528 of the export receptor Crm1. One of these compounds (i.e., 11) is currently under evaluation as a potential drug candidate for the treatment of certain types of cancer. These studies culminated in useful and path-pointing structure-activity relationships (SARs) that provide guidance for further improvements in the biological/pharmacological profiles of compounds within this class.
AB - A series of δ 12-prostaglandin J 3 (δ 12-PGJ 3) analogues and derivatives were synthesized employing an array of synthetic strategies developed specifically to render them readily available for biological investigations. The synthesized compounds were evaluated for their cytotoxicity against a number of cancer cell lines, revealing nanomolar potencies for a number of them against certain cancer cell lines. Four analogues (2, 11, 21, and 27) demonstrated inhibition of nuclear export through a covalent addition at Cys528 of the export receptor Crm1. One of these compounds (i.e., 11) is currently under evaluation as a potential drug candidate for the treatment of certain types of cancer. These studies culminated in useful and path-pointing structure-activity relationships (SARs) that provide guidance for further improvements in the biological/pharmacological profiles of compounds within this class.
UR - http://www.scopus.com/inward/record.url?scp=84971408252&partnerID=8YFLogxK
U2 - 10.1021/jacs.6b02075
DO - 10.1021/jacs.6b02075
M3 - Article
VL - 138
SP - 6550
EP - 6560
JO - Journal of the American Chemical Society
JF - Journal of the American Chemical Society
SN - 0002-7863
IS - 20
ER -