| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1392714 | European Journal of Medicinal Chemistry | 2013 | 7 Pages |
•A small library of structurally diverse α-aminophosphonates has been synthesized.•Synthesized compounds assayed for cytotoxic activity against human cancer cell lines.•Some of the compounds showed activity in micromolar range against some cell lines.•One compound showed high potency (IC50 value of 4 μM) against Jurkat cell line.•In one case, selectivity of activity of (R)- over (S)- was observed.
A small library of structurally diverse α-aminophosphonates has been synthesized by reacting alkyl/aryl aldehydes, alkyl/aryl amines and alkyl/aryl phosphites in one-pot catalyzed by Amberlite-IR 120 resin (acidic). All the synthesized α-aminophosphonates were assayed for their in vitro cytotoxic activities against a panel of five human cancer cell lines including A-549, NCI-H23 (Lung), Colo 320DM (Colon), MG-63 (Bone marrow) and Jurkat (Blood T lymphocytes). Compound 4n having (R)-1-phenylethanamine was found to be the most active amongst all the synthesized α-aminophosphonates against all the five cancer cell lines, most prominent being against Jurkat cell line with an IC50 value of 4 μM. Surprisingly, compound 4o having (S)-1-phenylethanamine was found to be devoid of any cytotoxicity. Our finding suggests that these chemical entities could further serve as interesting template for the design of potential anticancer agents.
Graphical abstractA small library of structurally diverse α-aminophosphonates has been synthesized and assayed for cytotoxic activity against human cancer cell lines. One compound showed high potency (IC50 of 4 μM) against Jurkat.Figure optionsDownload full-size imageDownload as PowerPoint slide
