期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 19, 页码 5756-5762出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.08.033
关键词
Central nervous system bioactivity; Antimalarial bioactivity; Cytotoxicity; Tunicate natural products; Synthetic derivatives of natural products
资金
- Office of Polar Programs of the National Science Foundation [ANT-0838776, ANT-0838773]
- National Institute of Mental Health [HHSN-271-2008-00025-C (NIMH PDSP)]
- Office of Polar Programs (OPP)
- Directorate For Geosciences [0838773] Funding Source: National Science Foundation
The marine invertebrate-derived meridianin A. the originally proposed structure for psammopemmin A. and several related 3-pyrimidylindole analogs were synthesized and subsequently investigated for central nervous system, antimalarial, and cytotoxic activity. A Suzuki coupling of an indoleborate ester to the pyrimidine electrophile was utilized to form the natural product and derivatives thereof. The 3-pyrimidineindoles were found to prevent radioligand binding to several CNS receptors and transporters, most notably, serotonin receptors (<0.2 mu M K-i for 5HT(2B)). Two compounds also inhibited the human malaria parasite Plasmodium falciparum (IC50 <50 mu M). Only the natural product was cytotoxic toward A549 cells (IC50 = 15 mu M). (C) 2011 Elsevier Ltd. All rights reserved.
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