Investigation of Heck coupling on 6-bromo[2,3-d]thienopyrimidines for construction of new EGFR inhibitor lead structures
| العنوان: | Investigation of Heck coupling on 6-bromo[2,3-d]thienopyrimidines for construction of new EGFR inhibitor lead structures |
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| المؤلفون: | F. Bysting, Bård Helge Hoff, Steffen Bugge, Eirik Sundby |
| المصدر: | 18569-18577 RSC Advances |
| بيانات النشر: | Royal Society of Chemistry, 2017. |
| سنة النشر: | 2017 |
| مصطلحات موضوعية: | 010405 organic chemistry, Stereochemistry, Chemistry, General Chemical Engineering, Egfr inhibition, chemistry.chemical_element, General Chemistry, Highly selective, 01 natural sciences, Combinatorial chemistry, 0104 chemical sciences, Catalysis, Solvent, 03 medical and health sciences, 0302 clinical medicine, 030220 oncology & carcinogenesis, Heck reaction, Isomerization, Palladium, EGFR inhibitors |
| الوصف: | With the aim of identifying new lead structures for EGFR inhibition, a study of palladium catalysed Heck coupling between (R)-6-bromo-N-(1-phenylethyl)thieno[2,3-d]pyrimidin-4-amine and various acrylates was performed. The Heck coupling was highly dependent on type of catalyst, solvent, base type and the use of tetrabutylammonium chloride as additive. The products were stable in the dark, but underwent trans–cis isomerization upon exposure to light. Kinase profiling indicate that acrylates grafted on the [2,3-d]thienopyrimidines is an attractive scaffold for identification of potent and highly selective EGFR inhibitors. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. |
| اللغة: | English |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d473c3d1194cfd47119afacadfae6a8Test https://hdl.handle.net/11250/2444444Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....4d473c3d1194cfd47119afacadfae6a8 |
| قاعدة البيانات: | OpenAIRE |
| الوصف غير متاح. |