Dual-acting 5-Fluorodeoxyuridine (FUdR) Prodrugs: Cell Death Induced by 3’-O-retinoyl-5-fluoro-2’-deoxyuridine and 5’-O-[bis(2,2,2,-trichloroethyl) phosphoryl-3’-O-butanoyl]-5-fluoro-2’-deoxyuridine
Bibliographic record
Abstract
Several novel 5-fluoro-2'-deoxyuridine (FUdR) prodrugs with postulated dual mechanisms of anticancer activity based on nucleoside cytotoxicity and cell differentiation induced by retinoic acid/butyric acid have been reported.The O-retinoyl-and O-butanoyl-esters of FUdR were reported to be more potent and had broader anticancer spectra than either FUdR or 5-fluorouracil (FU) against a bank of human cancer cell lines.The induction of necrosis or apoptosis in HL-60 cells by 3'-O-retinoyl-5-fluoro-2'-deoxyuridine (RFUdR) and the masked butyryl ester nucleotide, 5'-O-bis(trichloroethyl)phosphoryl-3'-O-butanoyl-5-fluoro-2'-deoxyuridine (BTCEP-BFUdR), is now reported.Apoptosis was the major pathway of HL-60 cell death caused by RFUdR (1 × 10 -5 M), independent of the exposure time.In contrast, apoptosis and necrosis were equally evident after exposure to BTCEP-BFUdR (1 × 10 -5 M) for 48 h, which is similar to the effect of FUdR.These in vitro data support a cytotoxicity model in which release of the nucleoside (FUdR) and the cell differentiator (all-trans retinoic acid, RA or butyrate, NaBu) from the respective prodrugs act synergistically to induce greater cell killing.
Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.
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) | 0.001 | 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".