Discovery and optimization of pyrazolopyrimidine sulfamates as ATG7 inhibitors
نویسندگان
چکیده
منابع مشابه
Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.
The identification and development of a novel series of small molecule Enhancer of Zeste Homologue 2 (EZH2) inhibitors is described. A concise and modular synthesis enabled the rapid development of structure-activity relationships, which led to the identification of 44 as a potent, SAM-competitive inhibitor of EZH2 that dose-dependently decreased global H3K27me3 in KARPAS-422 lymphoma cells.
متن کاملDesign, synthesis, and biological evaluation of novel carbohydrate-based sulfamates as carbonic anhydrase inhibitors.
Carbonic anhydrases (CAs) IX and XII are enzymes with newly validated potential for the development of personalized, first-in-class cancer chemotherapies. Here we present the design and synthesis of novel carbohydrate-based CA inhibitors, several of which were very efficient inhibitors (K(i)<10 nM) with good selectivity for cancer-associated CA isozymes over off-target CA isozymes. All inhibito...
متن کاملNew Pyrazolopyrimidine Inhibitors of Protein Kinase D as Potent Anticancer Agents for Prostate Cancer Cells
The emergence of protein kinase D (PKD) as a potential therapeutic target for several diseases including cancer has triggered the search for potent, selective, and cell-permeable small molecule inhibitors. In this study, we describe the identification, in vitro characterization, structure-activity analysis, and biological evaluation of a novel PKD inhibitory scaffold exemplified by 1-naphthyl P...
متن کاملDiscovery and Optimization of Inhibitors of DNA Methyltransferase as Novel Drugs for Cancer Therapy
The genome contains genetic and epigenetic information. While the genome provides the blueprint for the manufacture of all the proteins required to create a living thing, the epigenetic information provides instruction on how, where, and when the genetic information should be used (Robertson, 2001). The major form of epigenetic information in mammalian cells is DNA methylation that is the coval...
متن کاملStructure Optimization of Neuraminidase Inhibitors as Potential Anti-influenza (H1N1Inhibitors) Agents Using QSAR and Molecular Docking Studies
The urgent need of neuraminidase inhibitors (NI) has provided an impetus for understanding the structure requisite at molecular level. Our search for selective inhibitors of neuraminidase has led to the identification of pharmacophoric requirements at various positions around acyl thiourea pharmacophore. The main objective of present study is to develop selective NI, with least toxicity and dru...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2020
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2020.115681