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Synthesis and anticancer activities of novel (tetrahydrobenzo [4,5] thieno [2,3-d] pyrimidine-4-yl)-pyrolidine-2-carboxylic acid derivatives
被引:14
作者:
Pavase, Laxmikant S.
[1
]
Mane, Dhananjay V.
[1
]
机构:
[1] Dr Babasaheb Ambedkar Marathwada Univ, Dept Chem, Aurangabad 431004, Maharashtra, India
关键词:
Thieno pyrimidine;
Proline;
Gewald reaction;
MCF-7;
HCT-15;
Antitumor activities;
LUNG-CANCER;
AGENTS;
D O I:
10.1007/s00044-016-1692-x
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
Cancer chemotherapy has been one of the major medical advances in the last few decades. The medications involved in treatment have a narrow therapeutic index, and often the responses produced are only just palliative as well as unpredictable. In contrast, targeted therapy such as Tyrosine kinases inhibitors, that has been introduced in recent years is directed against cancer-specific molecules and signaling pathways with some side effects Therefore, we studied these class of molecules to obtain new candidates of remarkable activities and minimal side effects. We herein reported SAR driven synthesis of 16 novel molecules and their anticancer profiles in specifically targeted human Breast cell line MCF-7 and Human Colon Cancer Cell Line HCT-15. Compounds 7e and 8f showed descent antitumor activities when compared to Doxorubicine (GI(50) < 0.1) for human Breast cell line MCF-7. The synthesized analogs were ensured by spectral and elemental analysis.
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页码:2380 / 2391
页数:12
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