Abstract
These diterpenes (1) and (2) were synthesized via epoxidation and rearrangements of (-)-Kaur-9(11), 16-dien-19-oate (7) isolated from Venezuelan species of espeletia (frailejon), and their antimicrobial and antitumoral activity were evaluated. Compound (1) showed GI50 values of 51.6 nM against CNS SF-539, LC50 = 100 μM, log10 GI50 = -7.29; compound (2) showed GI50 at 4.17 μM against breast cancer T47D, LC50 = 39 μM and Log10 GI50 = -5.38. Our results suggest that these compounds are highly cytotoxic and cytostatic against human cancer cell lines.
Keywords: diterpene, kaurene, espeletia, antitumoral, cytostatic and cytotoxic
Letters in Drug Design & Discovery
Title: Cytostatic and Cytotoxic Activity of Synthetic Diterpene Derivatives Obtained from (-)-Kaur-9(11), 16-Dien-19-Oic Acid Against Human Cancer Cell Lines
Volume: 2 Issue: 4
Author(s): Randolph Alonso, Heidi Gomis, Antonieta Taddei and Cristina Sajo
Affiliation:
Keywords: diterpene, kaurene, espeletia, antitumoral, cytostatic and cytotoxic
Abstract: These diterpenes (1) and (2) were synthesized via epoxidation and rearrangements of (-)-Kaur-9(11), 16-dien-19-oate (7) isolated from Venezuelan species of espeletia (frailejon), and their antimicrobial and antitumoral activity were evaluated. Compound (1) showed GI50 values of 51.6 nM against CNS SF-539, LC50 = 100 μM, log10 GI50 = -7.29; compound (2) showed GI50 at 4.17 μM against breast cancer T47D, LC50 = 39 μM and Log10 GI50 = -5.38. Our results suggest that these compounds are highly cytotoxic and cytostatic against human cancer cell lines.
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Alonso Randolph, Gomis Heidi, Taddei Antonieta and Sajo Cristina, Cytostatic and Cytotoxic Activity of Synthetic Diterpene Derivatives Obtained from (-)-Kaur-9(11), 16-Dien-19-Oic Acid Against Human Cancer Cell Lines, Letters in Drug Design & Discovery 2005; 2 (4) . https://dx.doi.org/10.2174/1570180054038323
DOI https://dx.doi.org/10.2174/1570180054038323 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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