Synthesis of oxazoline hydroxamates α,β-unsaturated: Cytotoxic evaluation and inhibitory activity in vitro of histone deacetylases
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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How this classification was reachedexpand
Full frame machine prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.
Distilled classifier scores by category (both heads)
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.000 |
| 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) | 0.002 | 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 itClassification
machine, unvalidatedMachine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.
How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".