Synthesis and mechanistic aspects of 2-anilinonicotinyl-pyrazolo[1, 5-a]pyrimidine conjugates that regulate cell proliferation in MCF-7 cells via estrogen signaling. Issue 8 (15th April 2016)

• Record Type: Journal Article
• Authors: Kamal, Ahmed; Faazil, Shaikh; Hussaini, S.M. Ali; Ramaiah, M. Janaki; Balakrishna, M.; Patel, Nibedita; Pushpavalli, S.N.C.V.L.; Pal-Bhadra, Manika
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 8(2016)
• Page Start: 2077
• Page End: 2083
• Publication Date: 2016-04-15
• Subjects: Estrogen receptors -- Cell cycle -- Cyclin D1 -- Bcl-2 -- Pyrazolopyrimidine; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.02.072
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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 these6a and6c 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 compounds6a and6c reduced their activity.