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Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase.
TLDR
A novel fungal metabolite, apicidin, that exhibits potent, broad spectrum antiprotozoal activity in vitro against Apicomplexan parasites has been identified and is also orally and parenterally active in vivo against Plasmodium berghei malaria in mice.
Isolation, structure, and synthesis of combretastatins A-1 and B-1, potent new inhibitors of microtubule assembly, derived from Combretum caffrum.
TLDR
The structural simplicity and ready synthesis of combretastatin A-1 and combretastsatin B-1 suggest that these new biosynthetic products will become useful in a variety of biological endeavors.
Interactions of tubulin with potent natural and synthetic analogs of the antimitotic agent combretastatin: a structure-activity study.
TLDR
Available analogs were examined for antimitotic and cytotoxic activity and for effects on tubulin polymerization and colchicine binding and the most promising compound is the (cis)-stilbene derivative ( cis)-1-(3,4,5-trimethoxyphenyl)-2-(3'-hydroxy-4'-methoxyl)ethene, which has been named combretastatin A-4.
Isolation and structure of the strong cell growth and tubulin inhibitor combretastatin A-4
TLDR
The African treeCombretum caffrum (Combretaceae) has been found to contain a powerful inhibitor of tubulin polymerization (IC502–3 μM), the growth of murine lymphocytic leukemia and human colon cancer cell lines.
Solution conformation of the major adduct between the carcinogen (+)-anti-benzo[a]pyrene diol epoxide and DNA.
TLDR
The solution structure centered about the BP covalent adduct site in the (BP)G.C 11-mer duplex is determined by incorporating intramolecular and intermolecular proton-proton distance bounds deduced from the NMR data sets as constraints in energy minimization computations.
Selective inhibition of farnesyl-protein transferase blocks ras processing in vivo.
TLDR
These results are the first demonstration that a small organic chemical selected for inhibition of FPTase can inhibit Ras processing in vivo.
Antineoplastic agents, 120. Pancratium littorale.
TLDR
The bulbs of Pancratium littorale collected in Hawaii were found to contain a new phenanthridone biosynthetic product designated pancratistatin (4a) that proved to be effective against the murine P-388 lymphocytic leukemia.
Ophiobolin M and analogues, noncompetitive inhibitors of ivermectin binding with nematocidal activity.
TLDR
Ophiobolins which were most potent in the biological assays were also the most potent compounds when evaluated in a C. elegans motility assay, suggesting that the nematocidal activity of the ophiobolin is mediated via an interaction with the ivermectin binding site.
A novel antiviral agent which inhibits the endonuclease of influenza viruses
TLDR
A novel anti-influenza virus compound, flutimide, was identified in extracts of a recently identified fungal species, Delitschia confertaspora, and selectively inhibited the cap-dependent transcriptase of influenza A and B viruses and had no effect on the activities of other polymerases.
Isolation, structure, synthesis, and antimitotic properties of combretastatins B-3 and B-4 from Combretum caffrum.
TLDR
All the bibenzyls caused leukemia cells to accumulate in mitosis at cytotoxic drug concentrations; however, a wide range of in vitro activity against the protein tubulin (the major component of the mitotic spindle) was observed.
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