| Autor: |
Manpadi M; Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, New Mexico 87801, USA., Uglinskii PY, Rastogi SK, Cotter KM, Wong YS, Anderson LA, Ortega AJ, Van Slambrouck S, Steelant WF, Rogelj S, Tongwa P, Antipin MY, Magedov IV, Kornienko A |
| Jazyk: |
angličtina |
| Zdroj: |
Organic & biomolecular chemistry [Org Biomol Chem] 2007 Dec 07; Vol. 5 (23), pp. 3865-72. Date of Electronic Publication: 2007 Oct 24. |
| DOI: |
10.1039/b713820b |
| Abstrakt: |
A multicomponent reaction of indane-1,3-dione, an aldehyde and an amine-containing aromatic compound leading to the formation of indenopyridine-based heterocyclic medicinal scaffolds has been investigated. It was found that the yields significantly improve when oxygen gas is bubbled through the reaction mixture, facilitating the oxidation of the intermediate dihydropyridine-containing compounds to their aromatic counterparts. Investigation of the reaction scope revealed that formaldehyde, as well as various aliphatic, aromatic and heteroaromatic aldehydes, works well as the aldehyde component. In addition, substituted anilines and diverse aminoheterocycles can be utilized in this process as the amine-containing component. Preliminary biological evaluation of the synthesized library identified a pyrimidine-based polycycle, which rivals the anticancer drug etoposide in its toxicity and apoptosis inducing properties toward a human T-cell leukemia cell line. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
|
