Scopus
Synthesis of novel benzothiazole-piperazine derivatives and their biological evaluation as acetylcholinesterase inhibitors and cytotoxic agents
Anti-Cancer Agents in Medicinal Chemistry · Aralık 2017
Makale Bilgileri
DergiAnti-Cancer Agents in Medicinal Chemistry
Yayın TarihiAralık 2017
Cilt / Sayfa17 · 1837-1845
Scopus ID2-s2.0-85042775758
Özet
Objective and Method: A new series of benzothiazole-piperazine derivatives was synthesized and a complete chemical characterization of the novel compounds was provided. In vitro cytotoxic activities were screened against colorectal (HCT-116), breast (MCF-7) and hepatocellular (Huh7) cancer cell lines by Sulforhodamine B assay. Result and Discussion: All compounds showed cytotoxic activity against hepatocellular (Huh7) and breast (MCF-7) cancer cell lines. Dihalo substituted benzylpiperazine derivatives (2a, 2e) had the highest cytotoxic activities in all the tested cell lines. In addition, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of synthesized compounds were investigated by in vitro Ellman’s method. Compound 2j led to moderate and selective inhibition against AChE. Docking study was utilized to understand the binding mode of compound 2j in comparision with donepezil on AChE. The other tested compounds showed weak or no inhibition against AChE as promising anticancer agents.
Yazarlar (10)
1
Enise Ece Gurdal
2
Bengisu Turgutalp
3
Hayrettin Ozan Gulcan
4
Tugba Ercetin
5
Mustafa Şahin
6
Irem Durmaz
7
Rengul Cetin-Atalay
8
Quoc Dat Nguyen
9
Wolfgang Sippl
10
Mine Yarim
Anahtar Kelimeler
Acetylcholinesterase
Benzothiazole
Cytotoxicity
Docking
Ellman’s method
Piperazine
Sulforhodamine B
Kurumlar
Eastern Mediterranean University
Famagusta Turkey
Martin-Luther-Universität Halle-Wittenberg
Halle Germany
Middle East Technical University (METU)
Ankara Turkey
Yeditepe University
Istanbul Turkey
Metrikler
5
Atıf
10
Yazar
7
Anahtar Kelime