Synthesis of oxazoline hydroxamates α,β-unsaturated: Cytotoxic evaluation and inhibitory activity in vitro of histone deacetylases
Why this work is in the frame
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Bibliographic record
Abstract
A series of 28 molecules were synthesized: ten β-hydroxyamides, nine oxazoline esters, and nine oxazoline hydroxamates. Of these compounds, 16 represent new molecules. All synthesized compounds were evaluated against four cancer cell lines (MCF7, PC-3, NCI-H460, and HT-29) and one normal cell line (Vero). The results demonstrated that compound 4 h exhibited the highest activity, with an IC 50 of 7.65 μg/mL (24.67 μM) in PC-3 cells, which were determined to be the most sensitive cell line to the compounds. Because of this, the PC-3 cell line, as well as the Vero cell line, was chosen to evaluate the eventual inhibition of the HDAC enzyme by the most active oxazoline and hydroxamate ( 4 h and 5f , respectively) and to be able to analyze the possible mechanism of action exerted by these compounds. The inhibitory activity of HDAC produced by 4 h and 5f in PC-3 cells was found to be greater than that shown by the reference drug Vorinostat. In contrast, in Vero cells, the reference drug showed greater inhibitory activity than compounds 4 h and 5 f . These results suggest that compounds 4 h and 5f have greater selectivity towards HDAC cancer cells compared to normal growth cells; however, with less anticancer activity in vitro . • XtalFluor-E proved to be a good alternative for obtaining and oxazolines • In general, electron-withdrawing groups increase cytotoxic activity • Hydroxamates had promising cytotoxic activity but oxazoline esters were more active • 4 h and 5f had higher inhibition of HDAC in PC-3 cells compared to Vorinostat • In Vero cells, 4 h and 5f showed lesser suppression of HDAC activity than Vorinostat
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Full frame distilled prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.
Codex and Gemma teacher scores by category
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.001 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.000 |
| Insufficient payload (model declined to judge) | 0.000 | 0.000 |
Machine scores (provisional)
The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.
Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it