Discovery of potent T-type calcium channel blocker

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...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 17; no. 21; pp. 5740 - 5743
Main Authors Seo, Han Na, Choi, Ja Youn, Choe, Yun Jeong, Kim, Yoonjee, Rhim, Hyewhon, Lee, So Ha, Kim, Jungahn, Joo, Dong Jun, Lee, Jae Yeol
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 01.11.2007
Elsevier
Subjects
3,4-Dihydroquinazoline
Biological and medical sciences
Blocker
Calcium Channel Blockers - chemistry
Calcium Channel Blockers - pharmacology
Calcium Channels, T-Type - drug effects
Cardiovascular system
Cell Line
Humans
Kurtoxin
Medical sciences
Miscellaneous
Pharmacology. Drug treatments
Quinazolines - chemistry
Quinazolines - pharmacology
Structure-Activity Relationship
T-type calcium channel
Kurtoxin
Blocker
T-type calcium channel
3,4-Dihydroquinazoline
Nitrogen heterocycle
Calcium antagonist
Ionic channel
In vitro
Biphenyl derivatives
Tertiary amine
Bicyclic compound
Affinity
Carboxamide
Aromatic compound
Antagonist
Chemical synthesis
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Summary: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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.08.070