Show simple item record

dc.contributor.authorLutz, Vanessa
dc.contributor.authorMannchen, Fabian
dc.contributor.authorKrebs, Michael
dc.contributor.authorPark, Natja
dc.contributor.authorKrüger, Claudia
dc.contributor.authorRaja, Aruna
dc.contributor.authorSasse, Florenz
dc.contributor.authorBaro, Angelika
dc.contributor.authorLaschat, Sabine
dc.date.accessioned2017-02-08T13:16:01Z
dc.date.available2017-02-08T13:16:01Z
dc.date.issued2014-07-01
dc.identifier.citationSAR studies on hydropentalene derivatives--Important core units of biologically active tetramic acid macrolactams and ptychanolides. 2014, 22 (13):3252-61 Bioorg. Med. Chem.en
dc.identifier.issn1464-3391
dc.identifier.pmid24856181
dc.identifier.doi10.1016/j.bmc.2014.04.063
dc.identifier.urihttp://hdl.handle.net/10033/620813
dc.description.abstractStructurally diverse bicyclo[3.3.0]octanes were prepared and tested for their biological activity. Both the antiproliferative activity and the results of phenotypic characterization varied with the substitution patterns. Two derivatives displayed high inhibitory (IC50 ≤3μM) activity against the L-929 cell line, but differed in their mode of action. A cluster analysis with impedance profiling data showed the two compounds in relationship to microtubule interfering compounds. In PtK2 cells treated with both derivatives a perturbing effect on the microtubular network was observed, whereas the actin cytoskeleton in incubated PtK2 cells was disturbed only by one compound. The effects on tubulin and actin polymerization could be confirmed by in vitro polymerization experiments.
dc.language.isoenen
dc.rights.urihttp://creativecommons.org/licenses/by-nc-sa/4.0/*
dc.subject.meshAnimalsen
dc.subject.meshAntineoplastic Agentsen
dc.subject.meshBridged Bicyclo Compoundsen
dc.subject.meshCell Lineen
dc.subject.meshCell Proliferationen
dc.subject.meshDose-Response Relationship, Drugen
dc.subject.meshDrug Evaluation, Preclinicalen
dc.subject.meshHumansen
dc.subject.meshLactams, Macrocyclicen
dc.subject.meshMiceen
dc.subject.meshMolecular Conformationen
dc.subject.meshPyrrolidinonesen
dc.subject.meshStructure-Activity Relationshipen
dc.titleSAR studies on hydropentalene derivatives--Important core units of biologically active tetramic acid macrolactams and ptychanolides.en
dc.typeArticleen
dc.contributor.departmentHelmholtz Centre for infection research, Inhoffenstr. 7, 38124 Braunschweig, Germany.en
dc.identifier.journalBioorganic & medicinal chemistryen
refterms.dateFOA2018-06-13T05:30:20Z
html.description.abstractStructurally diverse bicyclo[3.3.0]octanes were prepared and tested for their biological activity. Both the antiproliferative activity and the results of phenotypic characterization varied with the substitution patterns. Two derivatives displayed high inhibitory (IC50 ≤3μM) activity against the L-929 cell line, but differed in their mode of action. A cluster analysis with impedance profiling data showed the two compounds in relationship to microtubule interfering compounds. In PtK2 cells treated with both derivatives a perturbing effect on the microtubular network was observed, whereas the actin cytoskeleton in incubated PtK2 cells was disturbed only by one compound. The effects on tubulin and actin polymerization could be confirmed by in vitro polymerization experiments.


Files in this item

Thumbnail
Name:
Publisher version
Thumbnail
Name:
Lutz et al.pdf
Size:
1.084Mb
Format:
PDF
Description:
original manuscript
Thumbnail
Name:
Supplementary data.pdf
Size:
1.319Mb
Format:
PDF
Description:
supplementary data

This item appears in the following Collection(s)

Show simple item record

http://creativecommons.org/licenses/by-nc-sa/4.0/
Except where otherwise noted, this item's license is described as http://creativecommons.org/licenses/by-nc-sa/4.0/