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Discovery of potent T-type calcium channel blocker.
Bioorg Med Chem Lett. 2007 Nov 01; 17(21):5740-3.BM

Abstract

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.

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Authors+Show Affiliations

Seo HN
Research Institute for Basic Sciences and Department of Chemistry, Kyung Hee University, Seoul 130-701, Republic of Korea.
Choi JY
No affiliation info available
Choe YJ
No affiliation info available
Kim Y
No affiliation info available
Rhim H
No affiliation info available
Lee SH
No affiliation info available
Kim J
No affiliation info available
Joo DJ
No affiliation info available
Lee JY
No affiliation info available

MeSH

Calcium Channel BlockersCalcium Channels, T-TypeCell LineHumansQuinazolinesStructure-Activity Relationship

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17869104

Citation

Seo, Han Na, et al. "Discovery of Potent T-type Calcium Channel Blocker." Bioorganic & Medicinal Chemistry Letters, vol. 17, no. 21, 2007, pp. 5740-3.
Seo HN, Choi JY, Choe YJ, et al. Discovery of potent T-type calcium channel blocker. Bioorg Med Chem Lett. 2007;17(21):5740-3.
Seo, H. N., Choi, J. Y., Choe, Y. J., Kim, Y., Rhim, H., Lee, S. H., Kim, J., Joo, D. J., & Lee, J. Y. (2007). Discovery of potent T-type calcium channel blocker. Bioorganic & Medicinal Chemistry Letters, 17(21), 5740-3.
Seo HN, et al. Discovery of Potent T-type Calcium Channel Blocker. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5740-3. PubMed PMID: 17869104.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Discovery of potent T-type calcium channel blocker. AU - Seo,Han Na, AU - Choi,Ja Youn, AU - Choe,Yun Jeong, AU - Kim,Yoonjee, AU - Rhim,Hyewhon, AU - Lee,So Ha, AU - Kim,Jungahn, AU - Joo,Dong Jun, AU - Lee,Jae Yeol, Y1 - 2007/09/01/ PY - 2007/05/18/received PY - 2007/08/16/revised PY - 2007/08/29/accepted PY - 2007/9/18/pubmed PY - 2008/2/6/medline PY - 2007/9/18/entrez SP - 5740 EP - 3 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 17 IS - 21 N2 - 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. SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/17869104/Discovery_of_potent_T_type_calcium_channel_blocker_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(07)01027-X DB - PRIME DP - Unbound Medicine ER -