1. Academic Validation
  2. Cinnamoyl compounds as simple molecules that inhibit p300 histone acetyltransferase

Cinnamoyl compounds as simple molecules that inhibit p300 histone acetyltransferase

  • J Med Chem. 2007 Apr 19;50(8):1973-7. doi: 10.1021/jm060943s.
Roberta Costi 1 Roberto Di Santo Marino Artico Gaetano Miele Paola Valentini Ettore Novellino Anna Cereseto
Affiliations

Affiliation

  • 1 Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Università di Roma La Sapienza, P.le A. Moro 5, I-00185 Roma, Italy.
Abstract

Cinnamoly compounds 1a-c and 2a-d were designed, synthesized, and in vitro tested as p300 inhibitors. At different degrees, all tested compounds were proven to inactivate p300, particularly, derivative 2c was the most active inhibitor, also showing high specificity for p300 as compared to other histone acetyltransferases. Most notably, 2c showed anti-acetylase activity in mammalian cells. These compounds represent a new class of synthetic inhibitors of p300, characterized by simple chemical structures.

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