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lH-Pyrazolo[3,4-b]quinolin-3-amine derivatives inhibit growth of colon cancer cells via apoptosis and sub G1 cell cycle arrest
Authors:Chandrabose Karthikeyan  Haneen Amawi  Arabela Guedes Viana  Leticia Sanglard  Noor Hussein  Maria Saddler  Charles R Ashby  NS Hari Narayana Moorthy  Piyush Trivedi  Amit K Tiwari
Institution:1. Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak 484887, India;2. Department of Pharmacology and Experimental Therapeutics, College of Pharmacy & Pharmaceutical Sciences, University of Toledo, OH, USA;3. Department of Biomedical Sciences, Tuskegee University, Tuskegee, AL, USA;4. College of Pharmacy and Pharmaceutical Sciences, St. John’s University, NY, USA;5. School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Bhopal 462036, India
Abstract:A series of lH-pyrazolo3,4-b]quinolin-3-amine derivatives were synthesized and evaluated for anticancer efficacy in a panel of ten cancer cell lines, including breast (MDAMB-231 and MCF-7), colon (HCT-116, HCT-15, HT-29 and LOVO), prostate (DU-145 and PC3), brain (LN-229), ovarian (A2780), and human embryonic kidney (HEK293) cells, a non-cancerous cell line. Among the eight derivatives screened, compound QTZ05 had the most potent and selective antitumor efficacy in the four colon cancer cell lines, with IC50 values ranging from 2.3 to 10.2?µM. Furthermore, QTZ05 inhibited colony formation in HCT-116 cells in a concentration-dependent manner. Cell cycle analysis data indicated that QTZ05 caused an arrest in the sub G1 cell cycle in HCT-116 cells. QTZ05 induced apoptosis in HCT-116 cells in a concentration-dependent manner that was characterized by chromatin condensation and increase in the fluorescence of fluorochrome-conjugated Annexin V. The findings from our study suggest that QTZ05 may be a valuable prototype for the development of chemotherapeutics targeting apoptotic pathways in colorectal cancer cells.
Keywords:Cytotoxicity  Colorectal cancer  Apoptosis
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