Name: 2,6-Dichloropurine. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. Author is Ma, Xiaodong; Wei, Jun; Wang, Chang; Gu, Dongyan; Hu, Yongzhou; Sheng, Rong.
A series of 24 benzothiadiazine derivatives I (R1 = Ph, 4-F-Ph, 3-CF3-Ph, etc; R2 = H, F, Cl; R3 = Me, Et; R4 = H, F, Cl), II, III (R5 = Ph, 4-F-Ph, 4-OCF3-Ph, 3-Py; R6 = H, F) with structural novelty were designed, synthesized and biol. evaluated as PI3Kδ-selective inhibitors. Structure-activity relationship (SAR) study showed that, compounds I (R1 = Ph; R2 = Cl; R3 = Et; R4 = H) and II (R2 = Cl; R3 = Me) were identified with single-digit nanomolar IC50 values against PI3Kδ and submicromolar GI50 values against human malignant B-cell line SU-DHL-6. Furthermore, chiral resolution of the key amine intermediate of these two compounds was performed to achieve corresponding enantiomers. Compounds (S)-3-(1-((9H-purin-6-yl)amino)ethyl)-8-chloro-2-phenyl-2Hbenzo[e][1,2,4]thiadiazine 1,1-dioxide(IC50: 4.6 nM) and (S)-4-amino-6-((1-(8-chloro-1,1-dioxido-2-phenyl-2H-benzo[e][1,2,4]thiadiazin-3-yl)ethyl)amino)pyrimidine-5-carbonitrile(IC50: below 0.32 nM) demonstrated comparable and superior PI3Kδ inhibitory activity, resp., to that of idelalisib. Addnl., both the compounds exerted enhanced anti-proliferative activity against the SU-DHL-6 cell line than that of idelalisib and they exhibited excellent PI3Kδ selectivity. The in vivo pharmacokinetic (PK) study revealed that (S)-3-(1-((9H-purin-6-yl)amino)ethyl)-8-chloro-2-phenyl-2Hbenzo[e][1,2,4]thiadiazine 1,1-dioxide displayed good plasma exposure and an acceptable oral bioavailability of 29.2% and can further be developed as a potential therapeutic agent for battling B-cell-mediated malignancies.
In some applications, this compound(5451-40-1)Name: 2,6-Dichloropurine is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.
Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem