Fioravanti, Rossella; Tomassi, Stefano; Bello, Elisabetta Di; Romanelli, Annalisa; Plateroti, Andrea Maria; Benedetti, Rosaria; Conte, Mariarosaria; Novellino, Ettore; Altucci, Lucia; Valente, Sergio; Mai, Antonello published the artcile< Properly substituted cyclic bis-(2-bromobenzylidene) compounds behaved as dual p300/CARM1 inhibitors and induced apoptosis in cancer cells>, Reference of 17082-09-6, the main research area is cyclic bisbromobenzylidene compound preparation diastereoselective antitumor activity; drug discovery; epigenetics; histone acetylation; histone methylation; multi-target agents.
The 1-benzyl-3,5-bis((E)-3-bromobenzylidene)piperidin-4-one displayed dual p300/EZH2 inhibition joined to cancer-selective cell death in a panel of tumor cells and in in-vivo xenograft models, a series of bis((E)-2-bromobenzylidene) cyclic compounds I (X = CH2) and I (X is NR, where R = H, Me, Bn, etc.) were prepared to test in biochem. (p300, PCAF, SIRT1/2, EZH2, and CARM1) and cellular (NB4, U937, MCF-7, SH-SY5Y) assays. The majority of I exhibited potent dual p300 and CARM1 inhibition, sometimes reaching the submicromolar level, and induction of apoptosis mainly in the tested leukemia cell lines. The most effective compounds in both enzyme and cellular assays carried a 4-piperidone moiety and a Me, benzyl, or acyl substituent at N1 position I [X is NR, where R = H, Me, Bn, 2-oxo-2-phenylethyl, 2-oxo-3-phenylpropyl, 2-oxo-4-phenylbutyl]. Elongation of the benzyl portion to I [X is NR, where R = 2-phenylethyl, 3-phenylpropyl] decreased the potency of compounds at both the enzymic and cellular levels, but the activity was promptly restored by introduction of a ketone group into the phenylalkyl substituent I [X is NR, where R = 2-oxo-2-phenylethyl, 3-oxo-3-phenylpropyl, 4-oxo-4-phenylbutyl]. Western blot analyses performed in NB4 and MCF-7 cells on selected compounds confirmed their inhibition of p300 and CARM1 through decrease of the levels of acetyl-H3 and acetyl-H4, marks for p300 inhibition, and of H3R17me2, mark for CARM1 inhibition.
Molecules published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 17082-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H7ClO, Reference of 17082-09-6.
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