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Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions.

National Cancer Institute-Bethesda
Neristatin 1 provides critical insight into bryostatin 1 structure-function relationships.

National Cancer Institute-Bethesda
Diacylglycerol lactones targeting the structural features that distinguish the atypical C1 domains of protein kinase C¿ and¿ from typical C1 domains.

National Cancer Institute-Bethesda
Methoxychalcone inhibitors of androgen receptor translocation and function.

National Cancer Institute-Bethesda
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.

National Cancer Institute-Bethesda
Depsides and depsidones as inhibitors of HIV-1 integrase: discovery of novel inhibitors through 3D database searching.

National Cancer Institute-Bethesda
HIV-1 integrase pharmacophore: discovery of inhibitors through three-dimensional database searching.

National Cancer Institute-Bethesda
Curcumin analogs with altered potencies against HIV-1 integrase as probes for biochemical mechanisms of drug action.

National Cancer Institute-Bethesda
Molecular modeling and site-directed mutagenesis studies of a phorbol ester-binding site in protein kinase C.

National Cancer Institute-Bethesda
Antiretroviral agents as inhibitors of both human immunodeficiency virus type 1 integrase and protease.

National Cancer Institute-Bethesda
Three-dimensional quantitative structure-activity relationship (QSAR) of HIV integrase inhibitors: a comparative molecular field analysis (CoMFA) study.

National Cancer Institute-Bethesda
4-Pregnen-21-ol-3,20-dione-21-(4-bromobenzenesulfonate) (NSC 88915) and related novel steroid derivatives as tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors.

National Cancer Institute-Bethesda
Azido-containing aryl beta-diketo acid HIV-1 integrase inhibitors.

National Cancer Institute-Bethesda
Conformationally constrained analogues of diacylglycerol (DAG). 17. Contrast between sn-1 and sn-2 DAG lactones in binding to protein kinase C.

National Cancer Institute-Bethesda
Examination of novel non-phosphorus-containing phosphotyrosyl mimetics against protein-tyrosine phosphatase-1B and demonstration of differential affinities toward Grb2 SH2 domains.

National Cancer Institute-Bethesda
Diacylglycerols with lipophilically equivalent branched acyl chains display high affinity for protein kinase C (PK-C). A direct measure of the effect of constraining the glycerol backbone in DAG lactones.

National Cancer Institute-Bethesda
Conformationally constrained analogues of diacylglycerol (DAG). 16. How much structural complexity is necessary for recognition and high binding affinity to protein kinase C?

National Cancer Institute-Bethesda
Inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands. 2. 4-(2-Malonyl)phenylalanine as a potent phosphotyrosyl mimetic.

National Cancer Institute-Bethesda
Significant compensatory role of position Y-2 conferring high affinity to non-phosphorylated inhibitors of Grb2-SH2 domain.

National Cancer Institute-Bethesda
Thiazolothiazepine inhibitors of HIV-1 integrase.

National Cancer Institute-Bethesda
Chicoric acid analogues as HIV-1 integrase inhibitors.

National Cancer Institute-Bethesda
Monocarboxylic-based phosphotyrosyl mimetics in the design of GRB2 SH2 domain inhibitors.

National Cancer Institute-Bethesda
Potent inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands.

National Cancer Institute-Bethesda
Potent inhibition of protein-tyrosine phosphatase-1B using the phosphotyrosyl mimetic fluoro-O-malonyl tyrosine (FOMT).

National Cancer Institute-Bethesda
Conformationally constrained analogues of diacylglycerol (DAG). 14. Dissection of the roles of the sn-1 and sn-2 carbonyls in DAG mimetics by isopharmacophore replacement.

National Cancer Institute-Bethesda
Salicylhydrazine-containing inhibitors of HIV-1 integrase: implication for a selective chelation in the integrase active site.

National Cancer Institute-Bethesda
Carbocyclic analogues of the potent cytidine deaminase inhibitor 1-(beta-D-ribofuranosyl)-1,2-dihydropyrimidin-2-one (zebularine).

National Cancer Institute-Bethesda
Arylamide inhibitors of HIV-1 integrase.

National Cancer Institute-Bethesda
Hydrazide-containing inhibitors of HIV-1 integrase.

National Cancer Institute-Bethesda
Discovery of HIV-1 integrase inhibitors by pharmacophore searching.

National Cancer Institute-Bethesda
Coumarin-based inhibitors of HIV integrase.

National Cancer Institute-Bethesda
Conformationally constrained analogues of diacylglycerol. 13. Protein kinase C ligands based on templates derived from 2,3-dideoxy-L-erythro(threo)-hexono-1,4-lactone and 2-deoxyapiolactone.

National Cancer Institute-Bethesda
4'-O-[2-(2-fluoromalonyl)]-L-tyrosine: a phosphotyrosyl mimic for the preparation of signal transduction inhibitory peptides.

National Cancer Institute-Bethesda
Conformationally constrained analogues of diacylglycerol. 12. Ultrapotent protein kinase C ligands based on a chiral 4,4-disubstituted heptono-1,4-lactone template.

National Cancer Institute-Bethesda
Conformationally constrained analogues of diacylglycerol. 11. Ultrapotent protein kinase C ligands based on a chiral 5-disubstituted tetrahydro-2-furanone template.

National Cancer Institute-Bethesda
Conformationally constrained analogues of diacylglycerol. 10. Ultrapotent protein kinase C ligands based on a racemic 5-disubstituted tetrahydro-2-furanone template.

National Cancer Institute-Bethesda
Bicyclic compounds as ring-constrained inhibitors of protein-tyrosine kinase p56lck.

National Cancer Institute-Bethesda
Protein kinase C. Modeling of the binding site and prediction of binding constants.

National Cancer Institute-Bethesda
The discovery of novel, structurally diverse protein kinase C agonists through computer 3D-database pharmacophore search. Molecular modeling studies.

National Cancer Institute-Bethesda
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides.

National Cancer Institute-Bethesda
Hydroxylated aromatic inhibitors of HIV-1 integrase.

National Cancer Institute-Bethesda
Phosphonate-containing inhibitors of tyrosine-specific protein kinases.

National Cancer Institute-Bethesda
Novel Radiolabeled Vanilloid with Enhanced Specificity for Human Transient Receptor Potential Vanilloid 1 (TRPV1).

National Cancer Institute-Bethesda
Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.

St. Jude Research Hospital
Quinuclidine derivatives and medicinal compositions containing the same

Almirall
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.

Hoffmann-La Roche