Synthesis of dimeric and tetrameric macrolactams with cytotoxic activity<sup>1</sup>
Bibliographic record
Abstract
Cyclization of amino acid 14, in turn prepared from 4,4-dimethylcyclohex-2-en-1-one by standard chemistry, yielded the dimeric and tetrameric macrolactams 15 and 16, respectively, representing the first examples of "taxoid-like" compounds with heterocyclic B rings. Compounds 15 and 16 exhibited moderate antiproliferative activity in an in vitro cytotoxicity assay. Consequently, an orthogonally diprotected, dimeric macrolactam 19 was synthesized and, after selective deprotection of the hydroxy group, was coupled with the docetaxel side chain to give the final compound 2, showing three-dimensional shape similarity to paclitaxel. Contrary to our expectations, 2 proved to be as active as the parent compound 15. The structure of 15 has been confirmed by X-ray crystallographic analysis and is also reported.Key words: macrolactams, macrocyclic compounds, taxane analogs, cytotoxic activity.
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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) | 0.001 | 0.001 |
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".