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.
Chiral aromatic heterocyclic amine derivative as well as synthesis method and application thereof
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Paragraph 0054; 0099; 0100; 0101; 0104; 0105; 0106; 0109, (2018/10/19)
The invention belongs to the technical field of compound synthesis, and specifically discloses a chiral aromatic heterocyclic amine derivative, as well as a synthesis method and application thereof. The chiral aromatic heterocyclic amine derivative has a structure represented by a formula (I), wherein R1 and R2 are independently selected from hydrogen or halogen; and R3 is an alkoxy group, a benzene ring, a methoxy group, an alkynyl group, a cyano group or a dihalogen substituted benzene ring, 5- or 6-membered heterocyclic ring, a methoxy group, an alkynyl group, a cyano group, a monohalogen or dihalogen substituted 5- or 6-membered heterocyclic ring, a fused heterocyclic ring; X is oxygen or nitrogen; Y is carbonyl or sulfonyl. The chiral aromatic heterocyclic amine derivative synthesizedby the invention have a function of inhibiting the assembly of the core protein of hepatitis B virus, can fundamentally inhibit the replication of hepatitis B virus, and have broad application prospects in the treatment of hepatitis B virus disease.
