Design and Synthesis of Tetrandrine Derivatives as Potential Anti‐tumor Agents Against A549 Cell Lines
Bibliographic record
Abstract
Abstract Tetrandrine ( 1 ) was converted to 5‐bromotetrandrine ( 2 ) using a mild oxidative system (DMSO/HBr). Suzuki‐Miyaura and Sonogashira cross‐coupling reactions were then employed to yield a set of 5‐substituted tetrandrine derivatives. A total of 19 new compounds was synthesized and they were characterized by 1 H NMR, 13 C NMR and HRMS. Their antiproliferative activities against A549 cell lines in vitro were evaluated using the MTT assay. Most of the compounds were found to possess significant inhibitory activities and compound 7 had the highest (IC 50 = 3.04 μM). Further studies on the mechanism demonstrated by compound 7 showed that it promotes apoptosis of A549 cells in a dose‐dependent manner and reduces the mitochondrial membrane potential. Western blot results showed that the compound up‐regulated the levels of Bax protein and down‐regulated the level of Bcl‐2 protein. Compared to the control group, the expression of cleaved‐caspase 3 and cleaved‐PARP in cells was significantly increased.
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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 | 0.000 |
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".