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1 article(s) from Hofstetter, Robert K.

Azologization and repurposing of a hetero-stilbene-based kinase inhibitor: towards the design of photoswitchable sirtuin inhibitors

Christoph W. Grathwol,
Nathalie Wössner,
Sören Swyter,
Adam C. Smith,
Enrico Tapavicza,
Robert K. Hofstetter,
Anja Bodtke,
Manfred Jung and
Andreas Link

Beilstein J. Org. Chem. 2019, 15, 2170–2183, doi:10.3762/bjoc.15.214

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Figure 1: Selisistat (1) and hit compound GW435821X (2a).

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Scheme 1: Reagents and conditions: a) appropriate boronic acid, Pd(PPh₃)₄, Na₂CO₃, DMF, H₂O, microwave, 15 mi...

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Scheme 2: Reagents and conditions: a) Pd₂(dba)₃ or Pd(OAc)₂, P(o-tol)₃, TEA, DMF, 120–140 °C, 0.7–24 h, 11–75...

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Figure 2: (Left) UV–vis spectrum of 2b 50 µM in 5% DMSO (v/v) in assay buffer after varying durations of irra...

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Figure 3: (Left) LC chromatogram of the LC–HRMS analysis of 2b after varying durations of irradiation with 25...

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Scheme 3: Photocyclization and oxidation reaction of 2b upon UV irradiation.

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Figure 4: Calculated and experimental absorption spectra of compounds (E)-2b-B (A), (Z)-2b-A (B), and product...

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Scheme 4: Reagents and conditions: a) 4-fluoroaniline, oxone, HAc, 60 °C, 14 d, 42%; b) NH₃, MeOH, rt, 3 d, 9...

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Figure 5: (Left) UV–vis spectrum of 11, 50 µM in 5% DMSO (v/v), in assay buffer at the thermal equilibrium an...

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Published 16 Sep 2019

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