Synthesis and preliminary mechanistic evaluation of N-(Substituted-1,3-Benzothiazol-2-yl)-2-(4- Substituted-Piperazin-1-yl) Acetamide derivatives with potent antiproliferative activity on human cancer cell lines

5^th World Congress on Cancer Therapy

September 28-30, 2015 Atlanta, USA

Mine Yarim1, Ece Gurdal, Irem Durmaz2 and Rengul Cetin-Atalay2

1Yeditepe University, Istanbul, Turkey
2Bilkent University, Ankara, Turkey

Scientific Tracks Abstracts: J Cancer Sci Ther

Abstract :

This lecture will cover synthesis, characterization and cytotoxic activities of some new benzothiazole-piperazine derivatives. Structures of compounds N-(substituted-1,3-benzothiazol-2-yl)-2-(4-substituted-piperazin-1-yl)acetamide derivatives were clarified with IR, 1H-NMR, 13C-NMR, mass spectroscopies and elemental analyses. In vitro cytotoxic activities of compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. Based on the GI50 values of the compounds, most of the benzothiazole-piperazine derivatives are active against HUH-7, MCF-7 and HCT-116 cancer cell lines. In addition, further investigation of compounds by Hoechst staining and FACS revealed that these compounds cause apoptosis by cell cycle arrest at subG1 phase. On the basis of their high potency in cellular environment, these straightforward benzothiazole-piperazine derivatives may possess potential in the design of more potent compounds for intervention with cancer cell proliferation.

Biography :

Yarim has completed his PhD from Hacettepe University and postdoctoral studies from ETH-Zürich. Professor Yarim has studied anticancer drug design and she has authored several peer-reviewed reports. She has served on numerous review committees for the National Science Foundation in Turkey. She has served on the editorial boards for the Pharmacologia. She is a member of the QSAR Society.

Email: myarim@yeditepe.edu.tr