Hu, Huiyong published the artcileDiscovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors, SDS of cas: 1260665-99-3, the main research area is preparation azaindazole pan Pim inhibitor antitumor neoplasm; crystal structure; Fragment based screen; Kinase inhibitor; Lead optimization; Pim kinases; Screening; Structure based drug design.
Pim kinase inhibitors are promising cancer therapeutics. Pim-2, among the three Pim isoforms, plays a critical role in multiple myeloma yet inhibition of Pim-2 is challenging due to its high affinity for ATP. A cocrystal structure of a screening hit I bound to Pim-1 kinase revealed the key binding interactions of its indazole core within the ATP binding site. Screening of analogous core fragments afforded 1H-pyrazolo[3,4-c]pyridine (6-azaindazole) as a core for the development of pan-Pim inhibitors. Fragment and structure based drug design led to identification of the series with picomolar biochem. potency against all three Pim isoforms. Desirable cellular potency was also achieved.
Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 1260665-99-3 belongs to class iodides-buliding-blocks, name is 3-Bromo-2-fluoro-6-iodopyridine, and the molecular formula is C5H2BrFIN, SDS of cas: 1260665-99-3.
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com