Design, synthesis and biological evaluation of <i>N</i>-pyridinyl ureidobenzenesulfonates and their hydrochloride salts as novel water-soluble dihydroorotate dehydrogenase inhibitors inducing differentiation of acute myeloid leukemia cells
Bibliographic record
Abstract
= 12-31 nM). In addition, molecular docking studies show their stable binding modes in the brequinar-binding site of DHODH. Furthermore, PYRUB-SOs trigger the differentiation of a significant portion of the population of both MOLM-13 and THP-1 cells, as evidenced by increased CD11b single expression and increased CD11b and CD14 dual expression, respectively. Finally, they exhibit metabolic stability with half-lives varying from 57 to 216 min in rodent and human liver microsomes. Our study highlights that the new PYRUB-SO salts improve the water solubility of this new family of DHODH inhibitors while maintaining their biological activity.
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How this classification was reachedexpand
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 | 0.001 | 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) | 0.000 | 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 itClassification
machine, unvalidatedMachine predicted; a candidate call from one teacher head, 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".