21363-10-0Relevant academic research and scientific papers
SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF NUCLEASES
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Page/Page column 14; 20-21, (2019/11/12)
The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3, R4, R5, R6 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
Structure–Activity Relationships on Cinnamoyl Derivatives as Inhibitors of p300 Histone Acetyltransferase
Madia, Valentina Noemi,Benedetti, Rosaria,Barreca, Maria Letizia,Ngo, Liza,Pescatori, Luca,Messore, Antonella,Pupo, Giovanni,Saccoliti, Francesco,Valente, Sergio,Mai, Antonello,Scipione, Luigi,Zheng, Yujun George,Tintori, Cristina,Botta, Maurizio,Cecchetti, Violetta,Altucci, Lucia,Di Santo, Roberto,Costi, Roberta
, p. 1359 - 1368 (2017/09/01)
Human p300 is a polyhedric transcriptional coactivator that plays a crucial role in acetylating histones on specific lysine residues. A great deal of evidence shows that p300 is involved in several diseases, including leukemia, tumors, and viral infection. Its involvement in pleiotropic biological roles and connections to diseases provide the rationale to determine how its modulation could represent an amenable drug target. Several p300 inhibitors (i.e., histone acetyltransferase inhibitors, HATis) have been described so far, but they all suffer from low potency, lack of specificity, or low cell permeability, which thus highlights the need to find more effective inhibitors. Our cinnamoyl derivative, 2,6-bis(3-bromo-4-hydroxybenzylidene)cyclohexanone (RC56), was identified as an active and selective p300 inhibitor and was proven to be a good hit candidate to investigate the structure–activity relationship toward p300. Herein, we describe the design, synthesis, and biological evaluation of new HATis structurally related to our hit; moreover, we investigate the interactions between p300 and the best-emerged hits by means of induced-fit docking and molecular-dynamics simulations, which provided insight into the peculiar chemical features that influence their activity toward the targeted enzyme.
Cu-catalyzed oxidative C(sp2)-H cycloetherification of o-arylphenols for the preparation of dibenzofurans
Zhao, Jiaji,Wang, Yong,He, Yimiao,Liu, Lanying,Zhu, Qiang
supporting information; experimental part, p. 1078 - 1081 (2012/03/27)
A new process involving copper-catalyzed aerobic C(sp2)-H activation, followed by cycloetherification, has been developed. This reaction serves as a direct method for the preparation of multisubstituted dibenzofurans starting with o-arylphenols. The presence of a strong para-electron-withdrawing group (e.g., NO2) on the phenol is essential for the success of the reaction.
CuI-mediated sequential iodination/cycloetherification of o-arylphenols: Synthesis of 2- or 4-iododibenzofurans and mechanistic studies
Zhao, Jiaji,Liu, Lanying,He, Yimiao,Li, Jing,Zhu, Qiang,Zhang, Qi,Li, Juan
supporting information, p. 5362 - 5365,4 (2012/12/12)
An efficient synthesis of 2- or 4-iododibenzofurans through CuI-mediated sequential iodination/cycloetherification of two aromatic C-H bonds in o-arylphenols has been developed. Both the preexisting electron-withdrawing groups (NO2, CN, and CHO) and the newly introduced iodide are readily modified for a focused dibenzofuran library synthesis. Mechanistic studies and DFT calculations suggest that a Cu(III)-mediated rate-limiting C-H activation step is involved in cycloetherification.
