Electric Literature of C5H2Cl2N4. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Scaffold hopping of the SYK inhibitor entospletinib leads to broader targeting of the BCR signalosome. Author is Jorda, Radek; Krajcovicova, Sona; Kralova, Petra; Soural, Miroslav; Krystof, Vladimir.
Spleen tyrosine kinase (SYK) and Bruton’s tyrosine kinase (BTK) are attractive targets in human haematol. malignancies with excessively activated B-cell receptor (BCR) signalling pathways. Entospletinib is a SYK inhibitor that has been evaluated as a clin. candidate. Design and synthesis of five isosteres in which the imidazo[1,2-a]pyrazine scaffold of entospletinib was altered to pyrazolo[3,4-d]pyrimidine, pyrrolo[3,2-d]pyrimidine, imidazo[4,5-b]pyridine, imidazo[4,5-c]pyridine and purine is reported. The last two isosteres were the most potent SYK inhibitors, with IC50 values in the mid-nanomolar range. Importantly, three compounds also inhibited BTK more effectively than did entospletinib. Further experiments then showed that BCR signalling was suppressed in Ramos cells by the potent compounds Preliminary kinase inhibition screening also revealed LCK and SRC as addnl. targets. These results further support the hypothesis that multikinase targeting compounds could produce more robust responses in the treatment of B lymphoid neoplasms.
Although many compounds look similar to this compound(5451-40-1)Electric Literature of C5H2Cl2N4, numerous studies have shown that this compound(SMILES:C2=NC1=C(C(=NC(=N1)Cl)Cl)[NH]2), has unique advantages. If you want to know more about similar compounds, you can read my other articles.
Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem