Synthesis and mechanistic aspects of 2-anilinonicotinyl-pyrazolo [1,5-a]pyrimidine conjugates that regulate cell proliferation in MCF-7 cells via estrogen signaling

被引：17

作者：

Kamal, Ahmed ^{[1
]}

Faazil, Shaikh ^{[1
]}

Hussaini, S. M. Ali ^{[1
,3
]}

Ramaiah, M. Janaki ^{[2
]}

Balakrishna, M. ^{[1
]}

Patel, Nibedita ^{[2
]}

Pushpavalli, S. N. C. V. L. ^{[2
]}

Pal-Bhadra, Manika ^{[2
]}

机构：

[1] Indian Inst Chem Technol, CSIR, Med Chem & Pharmacol, Hyderabad 500007, Andhra Pradesh, India

[2] Indian Inst Chem Technol, CSIR, Chem Biol Div, Hyderabad 500007, Andhra Pradesh, India

[3] Univ Saskatchewan, Dept Chem, 110 Sci Pl, Saskatoon, SK S7N 5C9, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 08期

关键词：

Estrogen receptors; Cell cycle; Cyclin D1; Bcl-2; Pyrazolopyrimidine; BREAST-CANCER; RECEPTOR-ALPHA; INHIBITORS; AGENTS; DERIVATIVES; EXPRESSION; BETA; APOPTOSIS; TUMORS;

D O I：

10.1016/j.bmcl.2016.02.072

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of anilinonicotinyl linked pyrazolo[1,5-a]pyrimidine conjugates (6a-x) were synthesized and evaluated for their antiproliferative activity. Some of these conjugates exhibited promising cytotoxic effects in the MCF-7 cell line and among these 6a and 6c exhibited significant effects, apart from G2/M cell cycle arrest. Interestingly they showed profound effects on cyclin D1, Bcl-2 and survivin proteins that regulate breast cancer cell proliferation. Moreover, ER alpha protein expression was studied to understand regulatory role of these conjugates on estrogen activity in estrogen positive breast cancer cells like MCF-7 and compounds 6a and 6c reduced their activity. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：2077 / 2083

页数：7

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