14000-67-0Relevant articles and documents
BIFUNCTIONAL COMPOUNDS FOR THE TREATMENT OF CANCER
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Page/Page column 57; 121-122, (2021/05/07)
The invention provides bifunctional compounds of formula (I) or a pharmaceutically acceptable salt thereof. Formula (I). The compounds cause the degradation of SMARCA2 via the targeted ubiquination of SMARCA2 protein and subsequent proteasomal degradation and are thus useful for the treatment of cancer. The targeting ligand is of formula (TL).
From PARP1 to TNKS2 inhibition: A structure-based approach
Tomassi, Stefano,Pfahler, Julian,Mautone, Nicola,Rovere, Annarita,Esposito, Chiara,Passeri, Daniela,Pellicciari, Roberto,Novellino, Ettore,Pannek, Martin,Steegborn, Clemens,Paiardini, Alessandro,Mai, Antonello,Rotili, Dante
supporting information, p. 862 - 868 (2020/06/30)
Tankyrases (TNKSs) have recently gained great consideration as potential targets in Wnt/β-catenin pathway-dependent solid tumors. Previously, we reported the 2-mercaptoquinazolin-4-one MC2050 as a micromolar PARP1 inhibitor. Here we show how the resolution of the X-ray structure of PARP1 in complex with MC2050, combined with the computational investigation of the structural differences between TNKSs and PARP1/2 active sites, provided the rationale for a structure-based drug design campaign that with a limited synthetic effort led to the discovery of the bis-quinazolinone 5 as a picomolar and selective TNKS2 inhibitor, endowed with antiproliferative effects in a colorectal cancer cell line (DLD-1) where the Wnt pathway is constitutively activated.
C26-LINKED RAPAMYCIN ANALOGS AS MTOR INHIBITORS
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Paragraph 00598, (2019/11/21)
The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.
