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Molecules 2014, 19(11), 18676-18689; doi:10.3390/molecules191118676

Design and Synthesis of Isosteviol Triazole Conjugates for Cancer Therapy

1
Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA
2
Department of Radiation Oncology, College of Medicine, University of Florida Health Cancer Center, Gainesville, FL 32610, USA
3
Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611, USA
Deceased on 10 February 2014.
*
Author to whom correspondence should be addressed.
Received: 13 October 2014 / Revised: 6 November 2014 / Accepted: 6 November 2014 / Published: 14 November 2014
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Abstract

One of the keys for successfully developing drugs against the broad spectrum of cancer cell types is structural diversity. In the current study, we focused on a family of isosteviol derivatives as potential novel antitumor agents. Isosteviol is a tetracyclic diterpenoid obtained by acid hydrolysis of steviol glycoside extracts isolated from abundant Stevia rebaudiana plants. In this work, we have designed and synthesized a panel of isosteviol triazole conjugates using “click” chemistry methodology. Evaluation of these compounds against a series of cancer cell lines derived from primary and metastatic tumors demonstrated that these conjugates exhibit cytotoxic activities with IC50 in the low μM range. In addition, their anti-proliferative activities are cancer cell type specific. Taken together, our studies underscore the importance of structural diversity in achieving cancer cell type specific drug development. View Full-Text
Keywords: isosteviol; triazole conjugates; anticancer activity; click chemistry isosteviol; triazole conjugates; anticancer activity; click chemistry
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MDPI and ACS Style

Khaybullin, R.N.; Zhang, M.; Fu, J.; Liang, X.; Li, T.; Katritzky, A.R.; Okunieff, P.; Qi, X. Design and Synthesis of Isosteviol Triazole Conjugates for Cancer Therapy. Molecules 2014, 19, 18676-18689.

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