New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes

Giuseppe Romeo; Luisa Materia; Gabriella Marucci; Maria Modica; Valeria Pittalà; Loredana Salerno; Maria Angela Siracusa; Michela Buccioni; Piero Angeli; Kenneth P Minneman

doi:10.1016/j.bmcl.2006.09.034

New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes

Bioorg Med Chem Lett. 2006 Dec 15;16(24):6200-3. doi: 10.1016/j.bmcl.2006.09.034. Epub 2006 Oct 5.

Authors

Giuseppe Romeo¹, Luisa Materia, Gabriella Marucci, Maria Modica, Valeria Pittalà, Loredana Salerno, Maria Angela Siracusa, Michela Buccioni, Piero Angeli, Kenneth P Minneman

Affiliation

¹ Dipartimento di Scienze Farmaceutiche, Università di Catania, viale A. Doria 6, 95125 Catania, Italy. [email protected]

PMID: 17027264
DOI: 10.1016/j.bmcl.2006.09.034

Abstract

A number of new pyrimido[5,4-b]indole and [1]benzothieno[3,2-d]pyrimidine derivatives were synthesized and evaluated for their binding and functional properties at alpha(1)-adrenergic receptor (alpha(1)-AR) subtypes. They behaved as potent alpha(1)-AR antagonists. In binding experiments, some of them (RC24 and RC23) showed very high affinity for the alpha(1D)-AR subtype.

Publication types

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

MeSH terms

Animals
Indoles / chemical synthesis
Indoles / metabolism*
Ligands
Male
Prostate / drug effects
Prostate / physiology
Pyrimidines / chemical synthesis
Pyrimidines / metabolism*
Rats
Receptors, Adrenergic, alpha-1 / physiology*
Structure-Activity Relationship

Substances

Indoles
Ligands
Pyrimidines
Receptors, Adrenergic, alpha-1