| Literature DB >> 19800245 |
Sucheta Kudrimoti1, Safwat A Ahmed, Pankaj R Daga, Amir E Wahba, Sherief I Khalifa, Robert J Doerksen, Mark T Hamann.
Abstract
Latrunculins are unique macrolides containing a thiazolidinone moiety. Latrunculins A, B and T and 16-epi-latrunculin B were isolated from the Red Sea sponge Negombata magnifica. N-Alkylated, O-methylated analogs of latrunculin B were synthesized and biological evaluation was performed for antifungal and antiprotozoal activity. The natural latrunculins showed significant bioactivity, while the semisynthetic analogs did not. Docking studies of these analogs into the X-ray crystal structure of G-actin showed that, in comparison with latrunculins A and B, N-alkylated latrunculins did not dock satisfactorily. This suggests that the analogs do not fit well into the active site of G-actin due to steric clashes and provides an explanation for the absence of bioactivity.Entities:
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Year: 2009 PMID： 19800245 PMCID： PMC2782694 DOI： 10.1016/j.bmc.2009.09.012
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641