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1 article(s) from Watkins, Davita L

Design and synthesis of diazine-based panobinostat analogues for HDAC8 inhibition

Sivaraman Balasubramaniam,
Sajith Vijayan,
Liam V. Goldman,
Xavier A. May,
Kyra Dodson,
Sweta Adhikari,
Fatima Rivas,
Davita L. Watkins and
Shana V. Stoddard

Beilstein J. Org. Chem. 2020, 16, 628–637, doi:10.3762/bjoc.16.59

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Figure 1: Chemical structures of the target diazine-based surrogates for the central core of panobinostat.

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Figure 2: Docking pose for panobinostat and panobinostat derivatives in the HDAC8 receptor. (a) Overlay of al...

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Figure 3: General building blocks for the visualized targets.

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Scheme 1: Reaction conditions: a) MeOH, H₂SO₄ (5 drops), MS 4 Å (2 pieces), 68 °C, 8 h, 81%; b) DIBAL-H (1.2 ...

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Scheme 2: Reaction conditions: a) boronic acid 15 (1.3 equiv), PdCl₂(PPh₃)₂ (0.1 equiv), dioxane/H₂O (3:1), Na...

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Scheme 3: Reaction conditions: a) 5-bromo-2-chloropyrimidine (1 equiv), ethyl formate (1.5 equiv), THF (20 mL...

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Scheme 4: Reaction conditions: a) boronic acid 15 (1.3 equiv), PdCl₂(PPh₃)₂ (0.1 equiv), dioxane/H₂O (8:2, Na₂...

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Published 07 Apr 2020

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