| Literature DB >> 20945914 |
Lingzhi Sun1, Falgun Shah, Mohamed A Helal, Yunshan Wu, Yakambram Pedduri, Amar G Chittiboyina, Jiri Gut, Philip J Rosenthal, Mitchell A Avery.
Abstract
Design and synthesis of a guaianolide-endoperoxide (thaperoxide) 3 was pursued as a new antimalarial lead which was found to be noncytotoxic as compared to the natural product lead thapsigargin 2. Several analogues of 3 were successfully synthesized and found to be comparable to derivatives of artemisinin 1 in in vitro antimalarial assay. Among the synthesized compounds, 22 showed excellent in vitro potency against the cultured parasites (W2 IC(50) = 13 nM) without apparent cytotoxicity. Furthermore, SAR trends in thaperoxide analogues are presented and explained with the help of docking studies in the homology model of PfSERCA(PfATP6).Entities:
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Year: 2010 PMID： 20945914 DOI： 10.1021/jm1006462
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446