التفاصيل البيبلوغرافية
العنوان:
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors
المؤلفون:
Steven C. Kim , Frederick Lee , Eileen Frommer , Mengxiao Shi , Yongbo Hu , Donald Wojciechowicz , Robert Mallon , Greg Ciszewski , Dan Maarten Berger , Karen Collins , Ariamala Gopalsamy , Larry Feldberg
المصدر:
Bioorganic & Medicinal Chemistry Letters . 19:6890-6892
بيانات النشر:
Elsevier BV, 2009.
سنة النشر:
2009
مصطلحات موضوعية:
Proto-Oncogene Proteins B-raf , Pyrimidine , Stereochemistry , medicine.drug_class , Clinical Biochemistry , Pharmaceutical Science , Antineoplastic Agents , Carboxamide , Biochemistry , chemistry.chemical_compound , Drug Discovery , medicine , Humans , Enzyme Inhibitors , Molecular Biology , chemistry.chemical_classification , biology , Kinase , Organic Chemistry , Hit to lead , Pyrimidines , Enzyme , chemistry , Enzyme inhibitor , Drug Design , biology.protein , Pyrazoles , Molecular Medicine , Signal transduction , Lead compound
الوصف:
Our continued effort towards optimization of the pyrazolo[1,5-a]pyrimidine scaffold as B-Raf kinase inhibitors is described. Structure guided design was utilized to introduce kinase hinge region interacting groups in the 2-position of the scaffold. This strategy led to the identification of lead compound 9 with enhanced enzyme and cellular potency, while maintaining good selectivity over a number of kinases.
تدمد:
0960-894X
الوصول الحر:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a6af29a6344c217dfecdc0daf235230Test https://doi.org/10.1016/j.bmcl.2009.10.074Test
حقوق:
CLOSED
رقم الانضمام:
edsair.doi.dedup.....9a6af29a6344c217dfecdc0daf235230
قاعدة البيانات:
OpenAIRE
