selected publications
- Indazole to 2-cyanoindole scaffold progression for mycobacterial lipoamide dehydrogenase inhibitors achieves extended target residence time and improved antibacterial activity. Angewandte Chemie (International ed. in English). 2024 Academic Article GET IT
- Nesprin-2 is a novel scaffold protein for telethonin and FHL-2 in the cardiomyocyte sarcomere. The Journal of biological chemistry. 2024 Academic Article GET IT
- Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055. ACS medicinal chemistry letters. 2024 Academic Article GET IT
- Addition to "Scaffold Hopping and Optimization of Small Molecule Soluble Adenyl Cyclase Inhibitors Led by Free Energy Perturbation". 2024 GET IT
- Scaffold Hopping and Optimization of Small Molecule Soluble Adenyl Cyclase Inhibitors Led by Free Energy Perturbation. Journal of chemical information and modeling. 2023 Academic Article GET IT
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On-demand male contraception via acute inhibition of soluble adenylyl cyclase.
Nature communications.
2023
Academic Article
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Times cited: 40 - Structure-Activity Relationship Studies of Antimalarial Plasmodium Proteasome Inhibitors─Part II. Journal of medicinal chemistry. 2023 Academic Article GET IT
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Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates.
Journal of medicinal chemistry.
2022
Academic Article
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Times cited: 10 -
Assessing potency and binding kinetics of soluble adenylyl cyclase (sAC) inhibitors to maximize therapeutic potential.
Frontiers in physiology.
2022
Academic Article
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Times cited: 6 - Small-molecule inhibition of the acyl-lysine reader ENL as a strategy against acute myeloid leukemia. Cancer discovery. 2022 Academic Article GET IT
- Design, Synthesis, and Optimization of Macrocyclic Peptides as Species-Selective Antimalaria Proteasome Inhibitors. Journal of medicinal chemistry. 2022 Academic Article GET IT
- Structure activity relationship of N-1 substituted 1,5-naphthyrid-2-one analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-9). Bioorganic & medicinal chemistry letters. 2022 Academic Article GET IT
- Transforming Academic Drug Discovery. Chembiochem : a European journal of chemical biology. 2022 Review GET IT
- A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors. ACS medicinal chemistry letters. 2022 Academic Article GET IT
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Soluble adenylyl cyclase inhibition prevents human sperm functions essential for fertilization.
Molecular human reproduction.
2021
Academic Article
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Times cited: 34 -
Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10).
ACS medicinal chemistry letters.
2021
Academic Article
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Times cited: 18 -
Macrocyclic Peptides that Selectively Inhibit the Mycobacterium tuberculosis Proteasome.
Journal of medicinal chemistry.
2021
Academic Article
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Times cited: 11 -
Development of a Highly Selective Plasmodium falciparum Proteasome Inhibitor with Anti-malaria Activity in Humanized Mice.
Angewandte Chemie (International ed. in English).
2021
Academic Article
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Times cited: 23 - Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules. Cancer research. 2021 Academic Article GET IT
- Whole Cell Active Inhibitors of Mycobacterial Lipoamide Dehydrogenase Afford Selectivity over the Human Enzyme through Tight Binding Interactions. ACS infectious diseases. 2021 Academic Article GET IT
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Optimization of lead compounds into on-demand, nonhormonal contraceptives: leveraging a public-private drug discovery institute collaboration†.
Biology of reproduction.
2020
Academic Article
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Times cited: 15 -
Selective Phenylimidazole-Based Inhibitors of the Mycobacterium tuberculosis Proteasome.
Journal of medicinal chemistry.
2019
Academic Article
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Times cited: 15 -
Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells.
Bioorganic & medicinal chemistry letters.
2019
Academic Article
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Times cited: 38 -
Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression.
Nature communications.
2019
Academic Article
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Times cited: 163 -
Improvement of Asparagine Ethylenediamines as Anti-malarial Plasmodium-Selective Proteasome Inhibitors.
Journal of medicinal chemistry.
2019
Academic Article
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Times cited: 29 -
Development of a New Structural Class of Broadly Acting HCV Non-Nucleoside Inhibitors Leading to the Discovery of MK-8876.
ChemMedChem.
2017
Academic Article
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Times cited: 8 -
Thiazomycin, nocathiacin and analogs show strong activity against clinical strains of drug-resistant Mycobacterium tuberculosis.
The Journal of antibiotics.
2017
Academic Article
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Times cited: 2 -
Alternative core development around the tetracyclic indole class of HCV NS5A inhibitors.
Bioorganic & medicinal chemistry letters.
2016
Academic Article
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Times cited: 10 -
In Vitro and In Vivo Characterization of the Novel Oxabicyclooctane-Linked Bacterial Topoisomerase Inhibitor AM-8722, a Selective, Potent Inhibitor of Bacterial DNA Gyrase.
Antimicrobial agents and chemotherapy.
2016
Academic Article
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Times cited: 22 -
Discovery of novel dihydrobenzofuran cyclopropane carboxylic acid based calcium sensing receptor antagonists for the treatment of osteoporosis.
Bioorganic & medicinal chemistry letters.
2016
Academic Article
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Times cited: 7 -
Discovery of fused tricyclic core containing HCV NS5A inhibitors with pan-genotype activity.
Bioorganic & medicinal chemistry letters.
2016
Academic Article
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Times cited: 13 -
Structure activity relationship of C-2 ether substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-5).
Bioorganic & medicinal chemistry letters.
2015
Academic Article
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Times cited: 11 -
Structure activity relationship of pyridoxazinone substituted RHS analogs of oxabicyclooctane-linked 1,5-naphthyridinyl novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-6).
Bioorganic & medicinal chemistry letters.
2015
Academic Article
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Times cited: 12 -
Hydroxy tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of RHS moiety (Part-3).
Bioorganic & medicinal chemistry letters.
2015
Academic Article
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Times cited: 17 -
Structure activity relationship of substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-4).
Bioorganic & medicinal chemistry letters.
2015
Academic Article
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Times cited: 14 -
Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety (Part-2).
Bioorganic & medicinal chemistry letters.
2015
Academic Article
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Times cited: 19 -
Design, synthesis, structure-function relationship, bioconversion, and pharmacokinetic evaluation of ertapenem prodrugs.
Journal of medicinal chemistry.
2014
Academic Article
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Times cited: 10 -
Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents.
ACS medicinal chemistry letters.
2014
Academic Article
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Times cited: 68 -
Discovery of MK-8742: an HCV NS5A inhibitor with broad genotype activity.
ChemMedChem.
2013
Academic Article
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Times cited: 174 -
Design, synthesis, and evaluation of prodrugs of ertapenem.
ACS medicinal chemistry letters.
2013
Academic Article
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Times cited: 7 -
Synthesis and antibacterial activity of novel water-soluble nocathiacin analogs.
Bioorganic & medicinal chemistry letters.
2012
Academic Article
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Times cited: 15 -
Novel transcriptome profiling analyses demonstrate that selective peroxisome proliferator-activated receptor γ (PPARγ) modulators display attenuated and selective gene regulatory activity in comparison with PPARγ full agonists.
Molecular pharmacology.
2012
Academic Article
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Times cited: 9 -
Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
Journal of medicinal chemistry.
2011
Academic Article
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Times cited: 41 -
Discovery of a pharmacologically active antagonist of the two-pore-domain potassium channel K2P9.1 (TASK-3).
ChemMedChem.
2011
Academic Article
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Times cited: 48 -
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.
Bioorganic & medicinal chemistry letters.
2009
Academic Article
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Times cited: 51 -
Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
Journal of medicinal chemistry.
2009
Academic Article
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Times cited: 20 -
Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus with a reduced potential to increase plasma and extracellular fluid volume.
Journal of medicinal chemistry.
2009
Academic Article
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Times cited: 44 -
Discovery of the development candidate N-tert-butyl nodulisporamide: a safe and efficacious once monthly oral agent for the control of fleas and ticks on companion animals.
Journal of medicinal chemistry.
2009
Academic Article
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Times cited: 25 -
Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides.
Bioorganic & medicinal chemistry letters.
2009
Academic Article
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Times cited: 23 -
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Bioorganic & medicinal chemistry letters.
2008
Academic Article
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Times cited: 14 -
Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice.
Diabetes.
2008
Academic Article
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Times cited: 154 -
A novel selective peroxisome proliferator-activator receptor-gamma modulator-SPPARgammaM5 improves insulin sensitivity with diminished adverse cardiovascular effects.
European journal of pharmacology.
2008
Academic Article
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Times cited: 30 -
Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Bioorganic & medicinal chemistry letters.
2008
Academic Article
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Times cited: 137 -
The differential interactions of peroxisome proliferator-activated receptor gamma ligands with Tyr473 is a physical basis for their unique biological activities.
Molecular pharmacology.
2007
Academic Article
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Times cited: 57 -
Conversion of nocathiacin I to nocathiacin acid by a mild and selective cleavage of dehydroalanine.
The Journal of organic chemistry.
2007
Academic Article
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Times cited: 18 -
A series of novel, potent, and selective histone deacetylase inhibitors.
Bioorganic & medicinal chemistry letters.
2006
Academic Article
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Times cited: 73 -
Design and synthesis of potent and subtype-selective PPARalpha agonists.
Bioorganic & medicinal chemistry letters.
2005
Academic Article
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Times cited: 18 -
Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
Bioorganic & medicinal chemistry letters.
2005
Academic Article
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Times cited: 58 -
Novel 2,3-dihydrobenzofuran-2-carboxylic acids: highly potent and subtype-selective PPARalpha agonists with potent hypolipidemic activity.
Journal of medicinal chemistry.
2005
Academic Article
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Times cited: 92 -
Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.
Bioorganic & medicinal chemistry letters.
2005
Academic Article
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Times cited: 20 -
Selective PPARgamma modulators with improved pharmacological profiles.
Bioorganic & medicinal chemistry letters.
2005
Academic Article
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Times cited: 67 -
PPARs: therapeutic targets for metabolic disease.
Trends in pharmacological sciences.
2005
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Times cited: 572 -
Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain.
Bioorganic & medicinal chemistry letters.
2005
Academic Article
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Times cited: 25 -
PPAR ligands: potential therapies for metabolic syndrome.
Current diabetes reports.
2005
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Times cited: 52 -
A disubstituted succinamide is a potent sodium channel blocker with efficacy in a rat pain model.
Biochemistry.
2004
Academic Article
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Times cited: 33 -
Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump.
The Journal of biological chemistry.
2003
Academic Article
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Times cited: 197 -
Nodulisporic acid side-chain modifications: access to the 2", 3", 4", and 6" registers.
Bioorganic & medicinal chemistry letters.
2003
Academic Article
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Times cited: 10 -
Side-chain homologation of nodulisporic acid: synthesis of potent new dienyl derivatives.
Bioorganic & medicinal chemistry letters.
2002
Academic Article
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Times cited: 8 -
Nodulisporic acid: its chemistry and biology.
Current topics in medicinal chemistry.
2002
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Times cited: 24 -
Lithocholic acid decreases expression of bile salt export pump through farnesoid X receptor antagonist activity.
The Journal of biological chemistry.
2002
Academic Article
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Times cited: 145 -
Ivermectin and nodulisporic acid receptors in Drosophila melanogaster contain both gamma-aminobutyric acid-gated Rdl and glutamate-gated GluCl alpha chloride channel subunits.
Biochemistry.
2002
Academic Article
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Times cited: 82 -
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.
Bioorganic & medicinal chemistry letters.
2002
Academic Article
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Times cited: 233 -
Synthesis of side chain truncated 3"-aldehyde, 3"-carboxylic acid, and 1"-aldehyde from nodulisporic acid A.
Organic letters.
2002
Academic Article
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Times cited: 9 -
Comparison of nodulisporic acid analogs in a Lucilia sericata in vitro assay and a Ctenocephalides felis membrane feeding system.
The Journal of parasitology.
2002
Academic Article
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Times cited: 6 -
Recent advances in the modulation of voltage-gated ion channels for the treatment of epilepsy.
Current drug targets. CNS and neurological disorders.
2002
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Times cited: 26 -
Synthesis of nodulisporic acid 2' '-oxazoles and 2' '-thiazoles.
Organic letters.
2001
Academic Article
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Times cited: 14 -
Systemic efficacy of nodulisporamides against fleas on dogs.
The Journal of parasitology.
2001
Academic Article
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Times cited: 15 -
Systemic activity of the avermectins against the cat flea (Siphonaptera: Pulicidae).
Journal of medical entomology.
2001
Academic Article
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Times cited: 22 -
Comparison of ivermectin, doramectin, selamectin, and eleven intermediates in a nematode larval development assay.
The Journal of parasitology.
2001
Academic Article
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Times cited: 31 -
Systemic efficacy of nodulisporic acid against fleas on dogs.
The Journal of parasitology.
2001
Academic Article
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Times cited: 40 -
Perspectives in animal health: old targets and new opportunities.
Journal of medicinal chemistry.
2001
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Times cited: 34 -
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1.
Bioorganic & medicinal chemistry letters.
2001
Academic Article
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Times cited: 71 -
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2.
Bioorganic & medicinal chemistry letters.
2001
Academic Article
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Times cited: 58 -
Synthesis of apicidin-derived quinolone derivatives: parasite-selective histone deacetylase inhibitors and antiproliferative agents.
Journal of medicinal chemistry.
2000
Academic Article
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Times cited: 59 -
Anticonvulsant and adverse effects of avermectin analogs in mice are mediated through the gamma-aminobutyric acid(A) receptor.
The Journal of pharmacology and experimental therapeutics.
2000
Academic Article
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Times cited: 98 -
Chemical modification of nodulisporic acid A: preliminary structure-activity relationships.
Bioorganic & medicinal chemistry letters.
2000
Academic Article
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Times cited: 20 -
Nodulisporic acid opens insect glutamate-gated chloride channels: identification of a new high affinity modulator.
Biochemistry.
2000
Academic Article
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Times cited: 61 -
Synthesis of gem-difluoro-avermectin derivatives: potent anthelmintic and anticonvulsant agents.
Bioorganic & medicinal chemistry letters.
1998
Academic Article
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Times cited: 10 - Synthesis of 1,19-Aza-1,19-desoxy-avermectin B(1a): The First Avermectin Macrolactam. The Journal of organic chemistry. 1998 Academic Article GET IT
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Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase.
Proceedings of the National Academy of Sciences of the United States of America.
1996
Academic Article
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Times cited: 539 -
Affinity probes for the avermectin binding proteins.
Journal of medicinal chemistry.
1992
Academic Article
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Times cited: 18 -
Photoaffinity labeling of avermectin binding sites from Caenorhabditis elegans and Drosophila melanogaster.
Proceedings of the National Academy of Sciences of the United States of America.
1992
Academic Article
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Times cited: 41