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.
Highlights
Natural products play a significant role in both chemical biology and drug discovery
In the current report we described the design and synthesis of novel isosteviol conjugates employing “click” chemistry for the purpose of new anticancer drug discovery
On the step isosteviol core was modified with alkyne functions to be suitable for “click” reaction
Summary
Natural products play a significant role in both chemical biology and drug discovery Their structural complexity enables natural small molecules to aim at a nearly limitless number of biological targets and often do so in a highly selective fashion [1]. Their great structural diversity along with numerous biological characteristics make natural compounds notably attractive both as promising therapeutic agents and a source for searching of new molecular entities with pharmacological activity [1,2,3]. In the current report we described the design and synthesis of novel isosteviol conjugates employing “click” chemistry for the purpose of new anticancer drug discovery
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