303122-55-6Relevant articles and documents
Structure–activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors
Fujii, Nobutaka,Honda, Maho,Kinoshita, Takayoshi,Minamiguchi, Daiki,Misu, Ryosuke,Moriwaki, Hirotomo,Nakamura, Shinya,Nakanishi, Isao,Nakanishi, Shinsuke,Ohno, Hiroaki,Oishi, Shinya,Okazaki, Shiho,Shu, Keito
, p. 1136 - 1141 (2016)
Two classes of modified analogs of 4-(thiazol-5-yl)benzoic acid-type CK2 inhibitors were designed. The azabenzene analogs, pyridine- and pyridazine-carboxylic acid derivatives, showed potent protein kinase CK2 inhibitory activities [IC50 (CK2α) = 0.014–0.017 μM; IC50 (CK2α′) = 0.0046–0.010 μM]. Introduction of a 2-halo- or 2-methoxy-benzyloxy group at the 3-position of the benzoic acid moiety maintained the potent CK2 inhibitory activities [IC50 (CK2α) = 0.014–0.016 μM; IC50 (CK2α′) = 0.0088–0.014 μM] and led to antiproliferative activities [CC50 (A549) = 1.5–3.3 μM] three to six times higher than those of the parent compound.
Aminothiazoles and aminothiadiazoles as nucleophiles in aminocarbonylation of iodobenzene derivatives
Gergely, Máté,Kollár, László
, p. 2030 - 2040 (2018/03/21)
Various 2-, 3- and 4-substituted iodobenzenes were aminocarbonylated using aminothiazole and aminothiadiazole derivatives in palladium-catalysed reaction. The reaction is chemospecific toward the corresponding carboxamides. Consequently, the application o
