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Molecules 2014, 19(11), 18676-18689;

Design and Synthesis of Isosteviol Triazole Conjugates for Cancer Therapy

Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA
Department of Radiation Oncology, College of Medicine, University of Florida Health Cancer Center, Gainesville, FL 32610, USA
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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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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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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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