380607-13-6Relevant articles and documents
From far west to east: Joining the molecular architecture of imidazole-like ligands in ho-1 complexes
Fallica, Antonino Nicolò,Floresta, Giuseppe,Greish, Khaled,Patamia, Vincenzo,Pittalà, Valeria,Rescifina, Antonio,Sorrenti, Valeria
, (2021/12/21)
HO-1 overexpression has been reported in several cases/types of human malignancies. Unfortunately, poor clinical outcomes are reported in most of these cases, and the inhibition of HO-1 is considered a valuable and proven anticancer approach. To identify
Synthesis, modeling, and RET protein kinase inhibitory activity of 3- and 4-substituted β-carbolin-1-ones
Cincinelli, Raffaella,Cassinelli, Giuliana,Dallavalle, Sabrina,Lanzi, Cinzia,Merlini, Lucio,Botta, Maurizio,Tuccinardi, Tiziano,Martinelli, Adriano,Penco, Sergio,Zunino, Franco
experimental part, p. 7777 - 7787 (2009/11/30)
A series of β-carbolin-2-ones and 3,10-dihydro-2H-azepino[3,4-b]indol- 1-ones have been designed, synthesized, and evaluated as RET protein kinase inhibitors on the basis of their structural similarity with the prototype indolin-2-one RPI-1. Some β-carbolin-2-ones (structure 2) showed an ability to inhibit RET enzymatic activity in vitro and proliferation of RETC634R oncogene-transformed NIH3T3 cells comparable to that of the reference compound. The docking analysis of the interaction of these compounds with the crystallographic structure of RET tyrosine kinase domain suggested a new binding interaction scheme different from the one proposed during their design. The rigid structure of the compounds of this series represents a new scaffold with potential advantages in the design of RET protein kinase inhibitors.
