Higher carbon analogues of 1,4-dihydropyridines as potent TGFβ/Smad inhibitors

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dc.contributor.authorBarth, Eva R.
dc.contributor.authorLängle, Daniel
dc.contributor.authorWesseler, Fabian
dc.contributor.authorGolz, Christopher
dc.contributor.authorKrupp, Anna
dc.contributor.authorSchade, Dennis
dc.contributor.authorStrohmann, Carsten
dc.date.accessioned2020-03-05T13:04:40Z
dc.date.available2020-03-05T13:04:40Z
dc.date.issued2019-11-20
dc.description.abstractThe C to Si and Ge exchange in bioactive compounds has often led to positive changes in the molecular properties, whereby Ge analogues are underrepresented. This is only possible at tetrahedral positions, and it is necessary for the analogue building blocks to withstand the synthetic conditions. Here, we present the synthesis of Si and Ge analogues of a TGFβ inhibiting 1,4‐dihydropyridine, which has a tetrahedral carbon in an important position for its activity. The molecular properties are compared by the discussion of the single X‐ray crystal structures and the electrostatic potential on the molecule surface which could play a role in the target interaction. Biological activities show that the C to Si and Ge exchange goes with full preservation of the potency, thus representing good starting points to modify physicochemical features and pharmacokinetics of these TGFβ inhibitors.en
dc.identifier.urihttp://hdl.handle.net/2003/39031
dc.identifier.urihttp://dx.doi.org/10.17877/DE290R-20950
dc.language.isoende
dc.relation.ispartofseriesEuropean Journal of Inorganic Chemistry;2020, Issue 2, S. 176-181
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.subjectBioisostersen
dc.subjectSiliconen
dc.subjectGermaniumen
dc.subject1,4-Dihydropyridinesen
dc.subjectTGF inhibitorsen
dc.subject.ddc540
dc.titleHigher carbon analogues of 1,4-dihydropyridines as potent TGFβ/Smad inhibitorsen
dc.typeTextde
dc.type.publicationtypearticlede
dcterms.accessRightsopen access
eldorado.secondarypublicationtruede
eldorado.secondarypublication.primarycitationEuropean journal of inorganic chemistry. 2020, Issue 2, 176-181de
eldorado.secondarypublication.primaryidentifierhttps://doi.org/10.1002/ejic.201901223de

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