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New aryl heteroaromatic compounds useful as tubulin polymerization inhibitors and tumor cell proliferation inhibitors
New aryl heteroaromatic compounds useful as tubulin polymerization inhibitors and tumor cell proliferation inhibitors
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机译：新的芳基杂芳族化合物可用作微管蛋白聚合抑制剂和肿瘤细胞增殖抑制剂
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摘要
Aryl heteroaromatic compounds (I) are new. Aryl heteroaromatic compounds of formula (I) and their isomers, prodrugs and salts are new. [Image] A : N or C; L1-G1-R1a piperazine residue of formula (i) or a 1,2,5,6-tetrahydropyridine residue of formula (ii); X, Y1CR3, N, NR3, O or S; E1CR4, N, NR4 or S; R1, R2optionally substituted aryl or heteroaryl; L1CO, CS or C=NR7; R3, R4H, alkyl, cycloalkyl, cycloalkenyl, heterocyclyl, OR7, SR7, SOR7, SO2R7, NR7R8, halo, aryl, heteroaryl, substituted cycloalkyl, substituted aryl or substituted heteroaryl; R5, R6H or 1-3C alkyl; and R7, R8H or optionally substituted 1-3C alkyl. Provided that (I) are not 1-phenyl-4-R2-3-(4-R1-1-piperazinecarbonyl)-1H-pyrazoles in which R1/R2 is 2-chlorophenyl/2-thienyl, 2-methoxyphenyl/2-thienyl, 2-methoxyphenyl/3,4-dimethoxyphenyl, 2-methoxyphenyl/3-pyridyl, 3-trifluoromethylphenyl/4-methoxyphenyl, 2-methoxyphenyl/4-chlorophenyl, phenyl/2-thienyl, phenyl/phenyl, 2-methoxyphenyl/4-fluorophenyl or phenyl/4-chlorophenyl, and (I) are not 1-(3-mesyl-2-naphthyl)-3-methyl-5-(4-(4-pyridyl)-1-piperazinecarbonyl)-1H-pyrazole, 1-phenyl-5-(4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinecarbonyl)-1H-pyrazole, 3-(4-fluorophenyl)-4-(4-phenyl-1-piperazinecarbonyl)-isoxazole or 3-phenyl-4-(4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinecarbonyl)-1,2,5-oxadiazole or its N-oxide or N,N-dioxide. [Image] ACTIVITY : Cytostatic; Antiarteriosclerotic. MECHANISM OF ACTION : Tubulin polymerization inhibitor; Tumor cell proliferation inhibitor. (4-(3-Chlorophenyl)-1-piperazinyl)-(1-phenyl-1H-imidazol-2-yl)-methanone had an IC50 of 2 mu M against tubulin polymerization and 0.0296 mu M against HCT116 cell proliferation.
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