European Journal of Medicinal Chemistry published new progress about Allosterism. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde.
Elkamhawy, Ahmed published the artcileDesign, synthesis and biological evaluation of novel thiazolidinedione derivatives as irreversible allosteric IKK-β modulators, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde, the main research area is benzylidene thiazolidinedione diastereoselective preparation antiinflammatory cytotoxicity allosteric IKKbeta modulator; thiazolidinedione benzaldehyde Knoevenagel condensation; Allosteric modulation; IKK-β modulators; NF-κB signaling pathway; Thiazolidinediones.
A series of thiazolidinedione-scaffold based chem. entities I [n = 3, 4, 5; R1 = 2-methoxyethyl, 3-methoxypropyl, cyclopropylmethyl, cyclopropanecarbonyl, methylsulfonyl; R2 = 4-(4-fluorophenoxy)phenyl, 4-(4-chlorophenoxy)phenyl, 4-(4-bromophenoxy)phenyl, 4-(4-nitrophenoxy)phenyl, 3-chloro-4-morpholino-phenyl] was synthesized and evaluated as potential allosteric covalent IKK-β modulators. Relative to the starting hit compound, derivatives I [n = 4, R1 = cyclopropylmethyl, R2 = 4-(4-nitrophenoxy)phenyl (II), 4-(4-fluorophenoxy)phenyl; n = 3, R1 = cyclopropylmethyl, R2 = 4-(4-nitrophenoxy)phenyl] elicited enhanced activity by 57-69 folds showing low micromolar IC50 values within the range of 1.4-1.7 mM. In addition, derivatives I [n = 5, R1 = cyclopropylmethyl, R2 = 4-(4-fluorophenoxy)phenyl (III), 3-chloro-4-morpholino-Ph; n = 3, R1 = cyclopropylmethyl, R2 = 3-chloro-4-morpholino-Ph (IV)] showed submicromolar IC50 values within the range of 0.4-0.9 mM, which was 243, 139 and 105 folds enhanced values. Kinetic study of compounds III and IV confirmed this class of modulators as irreversible inhibitors. Cellular assays presented compounds II and III as anti-inflammatory agents which suppressed both LPS-induced PGE2 and TNF-α production without non-specific cytotoxicity. Assay of hERG inhibition demonstrated a safe profile of compound II suggesting it as a lead for further development of IKK-β modulators.
European Journal of Medicinal Chemistry published new progress about Allosterism. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics