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Microwave-Assisted Synthesis of Potential Bioactive Benzo-, Pyrido- or Pyrazino-thieno[3,2- d ]pyrimidin-4-amine Analogs of MPC-6827.
- Source :
-
Pharmaceuticals (Basel, Switzerland) [Pharmaceuticals (Basel)] 2020 Aug 19; Vol. 13 (9). Date of Electronic Publication: 2020 Aug 19. - Publication Year :
- 2020
-
Abstract
- Efficient microwave-assisted chemical processes were applied to the synthesis of an array of novel N -(4-methoxyphenylamino)-2-methyl benzo-, pyrido- or pyrazino-thieno[3,2- d ]pyrimidin-4-amine derivatives. These heteroaromatic systems were envisioned as potent bioisosteric analogues of MPC-6827 , an anticancer agent previously developed until phase II clinical studies. A brief evaluation and comparison of their antiproliferative activity on HT-29 and Caco-2, two human colorectal cancer cell lines, were also reported. At the tested concentrations (5 and 10 µM), thieno[3,2- d ]pyrimidin-4-amines 4a and 4c exhibited an inhibitory effect similar to MPC-6827 on human colorectal cancer cell proliferation.
Details
- Language :
- English
- ISSN :
- 1424-8247
- Volume :
- 13
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Pharmaceuticals (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 32825171
- Full Text :
- https://doi.org/10.3390/ph13090202