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Communication

Microwave-Assisted Synthesis of Potential Bioactive Benzo-, Pyrido- or Pyrazino-thieno[3,2-d]pyrimidin-4-amine Analogs of MPC-6827

1
Normandie Univ, UNIROUEN, INSA Rouen, CNRS, COBRA UMR 6014, 76000 Rouen, France
2
Université de Nantes, Cibles et Médicaments des Infections et du Cancer, IICiMed, EA 1155, F-44000 Nantes, France
3
Normandie Univ, UNIROUEN, ABTE, 76000 Rouen, France
*
Authors to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(9), 202; https://0-doi-org.brum.beds.ac.uk/10.3390/ph13090202
Received: 25 July 2020 / Revised: 13 August 2020 / Accepted: 17 August 2020 / Published: 19 August 2020
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. View Full-Text
Keywords: microwave-assisted chemistry; thieno[3,2-d]pyrimidines; colorectal cancer; HT-29 cells; caco-2 cells; antiproliferative activity microwave-assisted chemistry; thieno[3,2-d]pyrimidines; colorectal cancer; HT-29 cells; caco-2 cells; antiproliferative activity
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MDPI and ACS Style

Loidreau, Y.; Nourrisson, M.-R.; Fruit, C.; Corbière, C.; Marchand, P.; Besson, T. Microwave-Assisted Synthesis of Potential Bioactive Benzo-, Pyrido- or Pyrazino-thieno[3,2-d]pyrimidin-4-amine Analogs of MPC-6827. Pharmaceuticals 2020, 13, 202. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13090202

AMA Style

Loidreau Y, Nourrisson M-R, Fruit C, Corbière C, Marchand P, Besson T. Microwave-Assisted Synthesis of Potential Bioactive Benzo-, Pyrido- or Pyrazino-thieno[3,2-d]pyrimidin-4-amine Analogs of MPC-6827. Pharmaceuticals. 2020; 13(9):202. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13090202

Chicago/Turabian Style

Loidreau, Yvonnick, Marie-Renée Nourrisson, Corinne Fruit, Cécile Corbière, Pascal Marchand, and Thierry Besson. 2020. "Microwave-Assisted Synthesis of Potential Bioactive Benzo-, Pyrido- or Pyrazino-thieno[3,2-d]pyrimidin-4-amine Analogs of MPC-6827" Pharmaceuticals 13, no. 9: 202. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13090202

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