التفاصيل البيبلوغرافية
العنوان:
Discovery of SARxxxx92, a pan-PIM kinase inhibitor, efficacious in a KG1 tumor model
المؤلفون:
Sachin Maniar , Anlai Wang , James Pribish , Shih-Min A. Huang , Andrew Hebert , Mikhail Levit , Jinyu Liu , Claude Barberis , Luke Fire , Elina Tserlin , Paul Erdman , Vinod F. Patel , Mark Czekaj , Joseph D. Batchelor , Frank Sun
المصدر:
Bioorganic & Medicinal Chemistry Letters . 30:127625
بيانات النشر:
Elsevier BV, 2020.
سنة النشر:
2020
مصطلحات موضوعية:
Indoles , Pyrrolidines , Clinical Biochemistry , hERG , Pharmaceutical Science , Antineoplastic Agents , Crystallography, X-Ray , 01 natural sciences , Biochemistry , Mice , Piperidines , Proto-Oncogene Proteins c-pim-1 , Cell Line, Tumor , Drug Discovery , medicine , Animals , Humans , Tumor growth , Protein Kinase Inhibitors , Molecular Biology , PK/PD models , Aza Compounds , biology , 010405 organic chemistry , Chemistry , Kinase , Organic Chemistry , Cancer , Stereoisomerism , medicine.disease , Xenograft Model Antitumor Assays , Rats , 0104 chemical sciences , 010404 medicinal & biomolecular chemistry , Permeability (electromagnetism) , biology.protein , Cancer research , Molecular Medicine , Tumor growth inhibition , Protein Binding
الوصف:
N-substituted azaindoles were discovered as potent pan-PIM inhibitors. Lead optimization, guided by structure and focused on physico-chemical properties allowed us to solve inherent hERG and permeability liabilities, and provided compound 27, which subsequently impacted KG-1 tumor growth in a mouse model.
تدمد:
0960-894X
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ec3a40682ad7fc0c9b4c038e0e32843 https://doi.org/10.1016/j.bmcl.2020.127625
حقوق:
CLOSED
رقم الأكسشن:
edsair.doi.dedup.....9ec3a40682ad7fc0c9b4c038e0e32843
قاعدة البيانات:
OpenAIRE
