Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase
Copyright © 2016 Elsevier Ltd. All rights reserved..
A group of small molecule thienopyrimidine inhibitors of Notum Pectinacetylesterase are described. We explored both 2-((5,6-thieno[2,3-d]pyrimidin-4-yl)thio)acetic acids and 2-((6,7-thieno[3,2-d]pyrimidin-4-yl)thio)acetic acids. In both series, highly potent, orally active Notum Pectinacetylesterase inhibitors were identified.
Medienart: |
E-Artikel |
---|
Erscheinungsjahr: |
2016 |
---|---|
Erschienen: |
2016 |
Enthalten in: |
Zur Gesamtaufnahme - volume:26 |
---|---|
Enthalten in: |
Bioorganic & medicinal chemistry letters - 26(2016), 6 vom: 15. März, Seite 1525-1528 |
Sprache: |
Englisch |
---|
Beteiligte Personen: |
Tarver, James E [VerfasserIn] |
---|
Links: |
---|
Anmerkungen: |
Date Completed 07.11.2016 Date Revised 28.07.2017 published: Print-Electronic Citation Status MEDLINE |
---|
doi: |
10.1016/j.bmcl.2016.02.021 |
---|
funding: |
|
---|---|
Förderinstitution / Projekttitel: |
|
PPN (Katalog-ID): |
NLM257675221 |
---|
LEADER | 01000naa a22002652 4500 | ||
---|---|---|---|
001 | NLM257675221 | ||
003 | DE-627 | ||
005 | 20231224183336.0 | ||
007 | cr uuu---uuuuu | ||
008 | 231224s2016 xx |||||o 00| ||eng c | ||
024 | 7 | |a 10.1016/j.bmcl.2016.02.021 |2 doi | |
028 | 5 | 2 | |a pubmed24n0858.xml |
035 | |a (DE-627)NLM257675221 | ||
035 | |a (NLM)26897593 | ||
035 | |a (PII)S0960-894X(16)30133-0 | ||
040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
041 | |a eng | ||
100 | 1 | |a Tarver, James E |c Jr |e verfasserin |4 aut | |
245 | 1 | 0 | |a Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase |
264 | 1 | |c 2016 | |
336 | |a Text |b txt |2 rdacontent | ||
337 | |a ƒaComputermedien |b c |2 rdamedia | ||
338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
500 | |a Date Completed 07.11.2016 | ||
500 | |a Date Revised 28.07.2017 | ||
500 | |a published: Print-Electronic | ||
500 | |a Citation Status MEDLINE | ||
520 | |a Copyright © 2016 Elsevier Ltd. All rights reserved. | ||
520 | |a A group of small molecule thienopyrimidine inhibitors of Notum Pectinacetylesterase are described. We explored both 2-((5,6-thieno[2,3-d]pyrimidin-4-yl)thio)acetic acids and 2-((6,7-thieno[3,2-d]pyrimidin-4-yl)thio)acetic acids. In both series, highly potent, orally active Notum Pectinacetylesterase inhibitors were identified | ||
650 | 4 | |a Journal Article | |
650 | 4 | |a Femur cortical bone thickness | |
650 | 4 | |a Notum Pectinacetylesterase | |
650 | 4 | |a Osteoporosis | |
650 | 4 | |a SAR | |
650 | 4 | |a Thienopyrimidine | |
650 | 7 | |a Enzyme Inhibitors |2 NLM | |
650 | 7 | |a Pyrimidines |2 NLM | |
650 | 7 | |a thienopyrimidine |2 NLM | |
650 | 7 | |a Esterases |2 NLM | |
650 | 7 | |a EC 3.1.- |2 NLM | |
650 | 7 | |a Notum protein, human |2 NLM | |
650 | 7 | |a EC 3.1.1.- |2 NLM | |
650 | 7 | |a Notum protein, mouse |2 NLM | |
650 | 7 | |a EC 3.1.1.- |2 NLM | |
700 | 1 | |a Pabba, Praveen K |e verfasserin |4 aut | |
700 | 1 | |a Barbosa, Joseph |e verfasserin |4 aut | |
700 | 1 | |a Han, Qiang |e verfasserin |4 aut | |
700 | 1 | |a Gardyan, Michael W |e verfasserin |4 aut | |
700 | 1 | |a Brommage, Robert |e verfasserin |4 aut | |
700 | 1 | |a Thompson, Andrea Y |e verfasserin |4 aut | |
700 | 1 | |a Schmidt, James M |e verfasserin |4 aut | |
700 | 1 | |a Wilson, Alan G E |e verfasserin |4 aut | |
700 | 1 | |a He, Wei |e verfasserin |4 aut | |
700 | 1 | |a Lombardo, Victoria K |e verfasserin |4 aut | |
700 | 1 | |a Carson, Kenneth G |e verfasserin |4 aut | |
773 | 0 | 8 | |i Enthalten in |t Bioorganic & medicinal chemistry letters |d 1992 |g 26(2016), 6 vom: 15. März, Seite 1525-1528 |w (DE-627)NLM09063828X |x 1464-3405 |7 nnns |
773 | 1 | 8 | |g volume:26 |g year:2016 |g number:6 |g day:15 |g month:03 |g pages:1525-1528 |
856 | 4 | 0 | |u http://dx.doi.org/10.1016/j.bmcl.2016.02.021 |3 Volltext |
912 | |a GBV_USEFLAG_A | ||
912 | |a GBV_NLM | ||
951 | |a AR | ||
952 | |d 26 |j 2016 |e 6 |b 15 |c 03 |h 1525-1528 |