Synthesis, evaluation of 6,8-dibromo-2-aryl-2,3-dihydroquinolin-4(1H)-ones in MCF-7 (breast cancer) cell lines and their docking studies

被引：17

作者：

Bheemanapalli, Lakshmi Narayana ^{[1
,2
]}

Kaur, Amandeep ^{[1
,2
]}

Arora, Ramandish ^{[1
,2
]}

Sangeeta ^{[1
,2
]}

Akkinepally, Raghuram Rao ^{[1
,2
]}

Javali, Narashima Murthy ^{[3
]}

机构：

[1] Panjab Univ, Pharmaceut Chem Div, Univ Inst Pharmaceut Sci, Chandigarh 160014, India

[2] Panjab Univ, Ctr Adv Study Pharmaceut Sci UGC CAS, Chandigarh 160014, India

[3] Univ Pacific, Dept Pharmaceut & Med Chem, Thomas J Long Sch Pharm & Hlth Sci, Stockton, CA 95211 USA

来源：

MEDICINAL CHEMISTRY RESEARCH | 2012年 / 21卷 / 08期

关键词：

Dihydroquinolin-4(1H)-ones; MCF-7 cell line; Nonsteroidal aromatase inhibitors; Docking studies; AROMATASE INHIBITORS; FLAVONOIDS;

D O I：

10.1007/s00044-011-9688-z

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 6,8-dibromo-2-aryl-2,3-dihydroquinolin-4(1H)-ones have been synthesized and evaluated in vitro (in MCF-7 breast cancer cell lines). Compounds 5a, 5d, 5e, and 5g exhibited potent GI(50) and TGI values compared with reference standard and compounds 5b and 5c showed moderate activity. The docking studies (in silico) were conducted to recognize the hypothetical binding motif of the title compounds within the active site of aromatase enzyme employing GOLD docking software. The binding mode and SAR of the title compounds has been proposed based on the docking studies.

引用

页码：1741 / 1750

页数：10

共 26 条

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[2]

[Anonymous], BREAST CANC FACTS FI

[3]

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[4]

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