Discovery of potent T-type calcium channel blocker

Autor:	Yun Jeong Choe, Han Na Seo, Jungahn Kim, So Ha Lee, Jae Yeol Lee, Yoonjee Kim, Dong Jun Joo, Ja Youn Choi, Hyewhon Rhim
Rok vydání:	2007
Předmět:	Tertiary amine medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Cell Line chemistry.chemical_compound Calcium Channels T-Type Structure-Activity Relationship Drug Discovery medicine Structure–activity relationship Potency Humans Molecular Biology Bicyclic molecule Calcium channel Organic Chemistry T-type calcium channel Calcium Channel Blockers chemistry Kurtoxin Quinazolines Molecular Medicine
Zdroj:	Bioorganicmedicinal chemistry letters. 17(21)
ISSN:	0960-894X
Popis:	The intensive SAR study of 3,4-dihydroquinazoline series led to the most potent compound 10 (KYS05090: IC(50)=41+/-1 nM) against T-type calcium channel and its potency is nearly comparable to that of Kurtoxin. As a small organic molecule, this compound showed the highest blocking activity reported to date.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2042796eeb3ea76e164bc4d8bcc2bb4 https://pubmed.ncbi.nlm.nih.gov/17869104 Zobrazit plný text záznamu Full Text from ScienceDirect