التفاصيل البيبلوغرافية
العنوان:
Discovery of N-substituted 7-azaindoles as Pan-PIM kinases inhibitors - Lead optimization - Part III
المؤلفون:
Andrew Hebert , Paul Erdman , Maniar Sachin , Anlai Wang , Alexandre Gross , Elina Tserlin , Claude Barberis , Vinod F. Patel , Jiang John Z , Mark Czekaj , Mikhail Levit , James Pribish , Frank Sun , Matthieu Barrague , Luke Fire , Shih-Min A. Huang
المصدر:
Bioorganicmedicinal chemistry letters . 29(3)
سنة النشر:
2018
مصطلحات موضوعية:
Indoles , Clinical Biochemistry , hERG , Compound 17 , Pharmaceutical Science , Antineoplastic Agents , 01 natural sciences , Biochemistry , Part iii , Mice , Structure-Activity Relationship , Proto-Oncogene Proteins c-pim-1 , Cell Line, Tumor , Drug Discovery , Animals , Humans , Molecular Biology , Protein Kinase Inhibitors , Cell Proliferation , biology , Dose-Response Relationship, Drug , Molecular Structure , 010405 organic chemistry , Chemistry , Organic Chemistry , Neoplasms, Experimental , Combinatorial chemistry , 0104 chemical sciences , Rats , 010404 medicinal & biomolecular chemistry , Pim kinases , biology.protein , Molecular Medicine , Tumor growth inhibition , Drug Screening Assays, Antitumor
الوصف:
N-substituted azaindoles were discovered as promising pan-PIM inhibitors. Lead optimization is described en route toward the identification of a clinical candidate. Modulation of physico-chemical properties allowed to solve inherent hERG and permeability liabilities. Compound 17 showed tumor growth inhibition in a KG1 tumor-bearing mouse model.
تدمد:
1464-3405
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c747e4800362180020faedb6eee28913 https://pubmed.ncbi.nlm.nih.gov/30553737
حقوق:
CLOSED
رقم الأكسشن:
edsair.doi.dedup.....c747e4800362180020faedb6eee28913
قاعدة البيانات:
OpenAIRE
