التفاصيل البيبلوغرافية
العنوان:
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists
المؤلفون:
Yanling Huang , Jingwu Duan , Carolyn A. Weigelt , Cullen L. Cavallaro , Javed Khan , Brian E. Fink , Muthoni G. Kamau , Zheming Ruan , Lan-Ying Qin , Sylwia Stachura , Cliff Chen , Murali Gururajan , Lalgudi S. Harikrishnan , Tram N. Huynh , John S. Sack , Anwar Murtaza , Daniel O'malley , Zhuyin Li , Melissa Yarde , Max Ruzanov , Virna Borowski , Patrice Gill , Huadong Sun , Zhonghui Lu , Jessica J. Wong
المصدر:
Bioorganicmedicinal chemistry letters . 30(12)
سنة النشر:
2020
مصطلحات موضوعية:
Agonist , Drug , medicine.drug_class , Receptors, Retinoic Acid , media_common.quotation_subject , Clinical Biochemistry , Retinoic acid , Pharmaceutical Science , Pharmacology , 01 natural sciences , Biochemistry , chemistry.chemical_compound , Mice , Structure-Activity Relationship , Pharmacokinetics , RAR-related orphan receptor gamma , Heterocyclic Compounds , Drug Discovery , Benzyl Compounds , medicine , Animals , Molecular Biology , media_common , Orphan receptor , chemistry.chemical_classification , Dose-Response Relationship, Drug , Molecular Structure , 010405 organic chemistry , Organic Chemistry , 0104 chemical sciences , Mice, Inbred C57BL , 010404 medicinal & biomolecular chemistry , chemistry , Pharmacodynamics , Molecular Medicine , Female , Tricyclic
الوصف:
Substituted benzyloxy aryl compound 2 was identified as an RORγt agonist. Structure based drug design efforts resulted in a potent and selective tricyclic compound 19 which, when administered orally in an MC38 mouse tumor model, demonstrated a desired pharmacokinetic profile as well as a dose-dependent pharmacodynamic response. However, no perceptible efficacy was observed in this tumor model at the doses investigated.
تدمد:
1464-3405
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d28391368dbe9fe0275182d85ed69ba6 https://pubmed.ncbi.nlm.nih.gov/32334911
حقوق:
CLOSED
رقم الأكسشن:
edsair.doi.dedup.....d28391368dbe9fe0275182d85ed69ba6
قاعدة البيانات:
OpenAIRE
