Synthesis and Biological Evaluation of Analogs of Didehydroepiandrosterone as Potential New Anticancer Agents
Abstract
:1. Introduction
2. Results
2.1. Chemistry
2.2. Biological Evaluation
3. Materials and Methods
3.1. Chemistry
3.1.1. General Methods
3.1.2. A General Procedure for the Deprotection
3.2. Biological Evaluation
3.2.1. Cell Studies
3.2.2. Protein Kinase Assay
4. Conclusions
Supplementary Materials
Author Contributions
Funding
Conflicts of Interest
References
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Sample Availability: Samples of the compounds 10a–10m are available from the authors. |
Compound | CEM Cell Assay IC50 (µM) a | HeLa Cell Assay IC50 (µM) a | HMEC-1 Cell Assay IC50 (µM) a | CDK8 Per Cent of Control (POC) |
---|---|---|---|---|
10a | >100 | >100 | >100 | n.d. b |
10b | 16 ± 3 | 90 ± 14 | 17 ± 4 | n.d. |
10c | 18 ± 4 | 97 ± 4 | 60 ± 4 | 95% |
10d | >100 | 2.1 ± 1.7 | 88 ± 8 | n.d. |
10e | 10 ± 1 | 18 ± 11 | 8.2 ± 1.9 | 100% |
10f | 24 ± 16 | 7.0 ± 2.5 | 11 ± 1 | n.d. |
10g | 14 ± 1 | 24 ± 6 | 15 ± 0 | n.d. |
10h | 16 ± 2 | 24 ± 8 | 13 ± 0 | 32% |
10i | 5.4 ± 0.6 | 9.2 ± 0.9 | 2.6 ± 0.4 | 100% |
10j | 5.8 ± 3.1 | 8.7 ± 0.0 | 5.4 ± 3.6 | 100% |
10k | 26 ± 17 | 91 ± 12 | 8.4 ± 4.3 | 100% |
10l | 1.5 ± 0.2 | 2.9 ± 1.0 | 0.59 ± 0.07 | 100% |
10m | 50 ± 21 | 44 ± 2 | 14 ± 2 | n.d. |
2-ME (3) | 1.6 ± 0.9 | 0.41 ± 0.06 | 1.3 ± 0.5 | n.d. |
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J. Solum, E.; Liekens, S.; Hansen, T.V. Synthesis and Biological Evaluation of Analogs of Didehydroepiandrosterone as Potential New Anticancer Agents. Molecules 2020, 25, 3052. https://doi.org/10.3390/molecules25133052
J. Solum E, Liekens S, Hansen TV. Synthesis and Biological Evaluation of Analogs of Didehydroepiandrosterone as Potential New Anticancer Agents. Molecules. 2020; 25(13):3052. https://doi.org/10.3390/molecules25133052
Chicago/Turabian StyleJ. Solum, Eirik, Sandra Liekens, and Trond Vidar Hansen. 2020. "Synthesis and Biological Evaluation of Analogs of Didehydroepiandrosterone as Potential New Anticancer Agents" Molecules 25, no. 13: 3052. https://doi.org/10.3390/molecules25133052