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Quinoline Consists of 1H-1,2,3-Triazole Hybrids: Design, Synthesis and Anticancer Evaluation
被引:15
作者:
Venkata, Sivarami Reddy Gangireddy
[1
,2
]
Narkhede, Umesh C.
[1
]
Jadhav, Vinod D.
[1
]
Naidu, Challa Gangu
[2
]
Addada, Ramakrishnam Raju
[1
]
Pulya, Sravani
[3
]
Ghosh, Balaram
[3
]
机构:
[1] GVK Biosci Pvt Ltd, Chem Serv, Hyderabad 500076, India
[2] VFSTRU, Dept Chem, Guntur 522213, Andhra Pradesh, India
[3] Birla Inst Technol & Sci, Dept Pharm, Hyderabad Campus, Hyderabad 500078, India
关键词:
Anticancer Evaluation;
CuAAC strategy;
Quinoline;
Suzuki coupling;
triazoles;
1,2,3-TRIAZOLES;
DERIVATIVES;
TRIAZOLE;
DOCKING;
D O I:
10.1002/slct.201903938
中图分类号:
O6 [化学];
学科分类号:
0703 ;
摘要:
A series of novel 8-bromo-1H-1,2,3-triazol-4-yl-2-methylquinoline derivatives and their Suzuki coupling products were synthesized via Copper catalyzed azide-alkyne cycloaddition (CuAAC) strategy followed by microwave assisted Suzuki coupling for the development of new series of anticancer agents. The invitro anticancer activity of the synthesized compounds were screened against human breast cancer (MDA-MB-231) and melanoma cell lines (B16F10). Among these, compounds 5 c (Azetidine), 5 e (Nitro benzoate), 5 f (fluorobenzyl)-1H-pyrazole), 5 g (Boc piperidine), 6 a (cyclo propyl), 6 c (5-fluoro-6-methoxypyridin-3-yl)and 6 d (2-methoxypyridin-3-yl) were showed anticancer activity ranging from 13.44 mu M to 38.2 mu M. The cellular toxicity of the novel compounds was also evaluated using normal human embryonic kidney (HEK) cell lines.
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页码:14184 / 14190
页数:7
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