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. 2018 May 6;23(5):1099. doi: 10.3390/molecules23051099

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© 2018 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).

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Scheme 1 — Preparation of novel histone H3 peptide-based LSD1 inactivators 2a–c with γ-turn inducers by Fmoc-based SPPS (Boc-Ala-OH was used as the N-terminal amino acid). Reagents and conditions: (a) MsCl, Et₃N in THF; (b) PCPA, Et₃N in H₂O:CH₃CN solution; (c) TFA, thioanisole, H₂O; and (d) preparative HPLC. Peptide chains shown in italics are protected.