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Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers.
Bioorg Med Chem Lett. 2005 Jan 17; 15(2):283-6.BM

Abstract

We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca(2+) channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca(2+) channels and N-type Ca(2+) channels. Among them, 5b (KYS05044, IC(50)=0.56+/-0.10 microM) was identified as potent T-type Ca(2+) channel blocker with in vitro selectivity profile at meaningful level (T/N-type, SI=>100).

Authors+Show Affiliations

Rhim H
Life Sciences Division, Korea Institute of Science & Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
Lee YS
No affiliation info available
Park SJ
No affiliation info available
Chung BY
No affiliation info available
Lee JY
No affiliation info available

MeSH

Calcium Channel BlockersCalcium Channels, N-TypeCalcium Channels, T-TypeCell LineInhibitory Concentration 50Molecular StructureOocytesQuinazolines

Pub Type(s)

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

Language

eng

PubMed ID

15603940

Citation

Rhim, Hyewhon, et al. "Synthesis and Biological Activity of 3,4-dihydroquinazolines for Selective T-type Ca2+ Channel Blockers." Bioorganic & Medicinal Chemistry Letters, vol. 15, no. 2, 2005, pp. 283-6.
Rhim H, Lee YS, Park SJ, et al. Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers. Bioorg Med Chem Lett. 2005;15(2):283-6.
Rhim, H., Lee, Y. S., Park, S. J., Chung, B. Y., & Lee, J. Y. (2005). Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers. Bioorganic & Medicinal Chemistry Letters, 15(2), 283-6.
Rhim H, et al. Synthesis and Biological Activity of 3,4-dihydroquinazolines for Selective T-type Ca2+ Channel Blockers. Bioorg Med Chem Lett. 2005 Jan 17;15(2):283-6. PubMed PMID: 15603940.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers. AU - Rhim,Hyewhon, AU - Lee,Yong Sup, AU - Park,Seong Jun, AU - Chung,Bong Young, AU - Lee,Jae Yeol, PY - 2004/09/16/received PY - 2004/10/28/accepted PY - 2004/12/18/pubmed PY - 2005/6/29/medline PY - 2004/12/18/entrez SP - 283 EP - 6 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 15 IS - 2 N2 - We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca(2+) channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca(2+) channels and N-type Ca(2+) channels. Among them, 5b (KYS05044, IC(50)=0.56+/-0.10 microM) was identified as potent T-type Ca(2+) channel blocker with in vitro selectivity profile at meaningful level (T/N-type, SI=>100). SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/15603940/Synthesis_and_biological_activity_of_34_dihydroquinazolines_for_selective_T_type_Ca2+_channel_blockers_ DB - PRIME DP - Unbound Medicine ER -