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Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex.
TLDR
X-ray crystal structures of the human top1-DNA complex bound with camptothecin and representative members of the indenoisoquinoline and indolocarbazole classes of top1 poisons are reported to aid the rational design of completely novel structural classes of anticancer drugs. Expand
Synthesis, antitubulin and antimitotic activity, and cytotoxicity of analogs of 2-methoxyestradiol, an endogenous mammalian metabolite of estradiol that inhibits tubulin polymerization by binding to
TLDR
The potencies of the analogs as cytotoxic and antimitotic agents in cancer cell cultures correlated with their potencies as inhibitors of tubulin polymerization, supporting the hypothesis that inhibition of tubul polymerization is the mechanism of the cytotoxicity action of 2-methoxyestradiol and its congeners. Expand
Selective synthesis and biological evaluation of sulfate-conjugated resveratrol metabolites.
TLDR
Resveratrol sulfates displayed low antiproliferative activity and negligible uptake in MCF7 cells, and its 3'-sulfate and 4-sulfates inhibit NO production by NO scavenging and down-regulation of iNOS expression in RAW 264.7 cells. Expand
Estrogenic effects of resveratrol in breast cancer cells expressing mutant and wild-type estrogen receptors: role of AF-1 and AF-2
TLDR
The effect of modifying or deleting AF domains depends strongly on the ligand and the target gene, and on cells carrying a stably integrated reporter gene, indicating that this phenomenon is not a result of transient transfection. Expand
Novel indenoisoquinolines NSC 725776 and NSC 724998 produce persistent topoisomerase I cleavage complexes and overcome multidrug resistance.
TLDR
Indenoisoquinoline derivatives are synthesized as novel topoisomerase I (Top1) inhibitors and induce Top1 cleavage at unique genomic positions compared with CPT, and show cross-resistance in cells deficient or silenced for Top1, which is consistent with their selective Top1 targeting. Expand
Synthesis and evaluation of analogues of (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene as potential cytotoxic and antimitotic agents.
TLDR
A series of stilbenes prepared and tested for cytotoxicity in the five human cancer cell lines A-549 non-small cell lung, MCF-7 breast, HT-29 colon, SKMEL-5 melanoma, and MLM melanoma proved to be cytotoxic in all five cell lines, with potencies comparable to that of combretastatin A-4. Expand
Preparation and anti-HIV activities of aurintricarboxylic acid fractions and analogues: direct correlation of antiviral potency with molecular weight.
TLDR
Results on the ATA fractions indicate that the binding of ATA to gp120 in the absence of CD4 binding is sufficient for anti-HIV activity, which is due to inhibition of virus binding due to an interference with the gp120-CD4 interaction. Expand
The indenoisoquinoline noncamptothecin topoisomerase I inhibitors: update and perspectives
TLDR
The use of γ-H2AX as a pharmacodynamic biomarker for the clinical development of the indenoisoquinolines is discussed, which results in the rapid and sustained phosphorylation of histone H2AX. Expand
The atomic structure of pentameric lumazine synthase from Saccharomyces cerevisiae at 1.85 A resolution reveals the binding mode of a phosphonate intermediate analogue.
TLDR
The data enable the reconstruction of the reactant topology during the early steps of the catalytic reaction, and structural determinants, which are likely to be responsible for the inability of the S. cerevisiae enzyme to form icosahedral capsids, will be discussed. Expand
Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction.
TLDR
Although cosalane inhibits HIV-1 reverse transcriptase and protease, time of addition experiments indicate that it prevents the cytopathic effect of HIV by acting earlier than reverse transcription in the viral replication cycle. Expand
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