Bioorganic & medicinal chemistry letters

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Design and Biophysical Characterization of Second-Generation cyclic peptide LAG-3 inhibitors for cancer immunotherapy.. 113. 2024
Stability studies of β-Amino- and β-Hydroxy difluoromethyl ketones in rat serum and rat liver microsomes. 2024
Design and synthesis of a library of C8-substituted sulfamidoadenosines to probe bacterial permeability.. 110. 2024
Design of cyclic peptides as novel inhibitors of ICOS/ICOSL interaction. 2024
Design and Synthesis of a Library of C2-Substituted Sulfamidoadenosines to Probe Bacterial Permeability. 2023
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). 2022
Topoisomerase IIα inhibitory and antiproliferative activity of dihydroxylated 2,6-diphenyl-4-fluorophenylpyridines: Design, synthesis, and structure-activity relationships.. 60. 2022
Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.. 57. 2021
Discovery of biphenyl pyrazole scaffold for neurodegenerative diseases: A novel class of acetylcholinesterase-centered multitargeted ligands.. 30. 2020
Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells.. 29. 2019
Quinoline and thiazolopyridine allosteric inhibitors of MALT1.. 29. 2019
Peptide-based covalent inhibitors of MALT1 paracaspase.. 29. 2019
A novel tetrazole analogue of resveratrol is a potent anticancer agent.. 29. 2018
Structure-based design, synthesis, and evaluation of structurally rigid donepezil analogues as dual AChE and BACE-1 inhibitors.. 28. 2018
Modular synthesis of new C-aryl-nucleosides and their anti-CML activity.. 28. 2018
Design, synthesis, and biological evaluation of α-hydroxyacyl-AMS inhibitors of amino acid adenylation enzymes.. 26. 2016
Alternative core development around the tetracyclic indole class of HCV NS5A inhibitors.. 26. 2016
Discovery of novel dihydrobenzofuran cyclopropane carboxylic acid based calcium sensing receptor antagonists for the treatment of osteoporosis.. 26. 2016
Discovery of fused tricyclic core containing HCV NS5A inhibitors with pan-genotype activity.. 26. 2016
Design, synthesis, and analysis of antagonists of GPR55: Piperidine-substituted 1,3,4-oxadiazol-2-ones.. 26. 2016
Cheminformatic comparison of approved drugs from natural product versus synthetic origins.. 25. 2015
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).. 25. 2015
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).. 25. 2015
Potent benzoazepinone γ-secretase modulators with improved bioavailability.. 25. 2015
Hydroxy tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of RHS moiety (Part-3).. 25. 2015
Structure activity relationship of substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-4).. 25. 2015
Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety (Part-2).. 25. 2015
Undesired versus designed enzymatic cleavage of linkers for liver targeting.. 24. 2014
Dactyloditerpenol acetate, a new prenylbisabolane-type diterpene from Aplysia dactylomela with significant in vitro anti-neuroinflammatory activity.. 24. 2013
Sandmeyer reaction repurposed for the site-selective, non-oxidizing radioiodination of fully-deprotected peptides: studies on the endogenous opioid peptide α-neoendorphin.. 23. 2013
Synthesis and antibacterial activity of novel water-soluble nocathiacin analogs.. 23. 2012
Synthesis and biological evaluation of novel technetium-99m labeled phenylbenzoxazole derivatives as potential imaging probes for β-amyloid plaques in brain.. 22. 2012
The co-crystal structure of ubiquitin carboxy-terminal hydrolase L1 (UCHL1) with a tripeptide fluoromethyl ketone (Z-VAE(OMe)-FMK).. 22. 2012
Cyclic amino acid linkers stabilizing key loops of brain derived neurotrophic factor.. 22. 2011
Chemical scaffolds with structural similarities to siderophores of nonribosomal peptide-polyketide origin as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis.. 21. 2011
Synthesis of purine-scaffold fluorescent probes for heat shock protein 90 with use in flow cytometry and fluorescence microscopy.. 21. 2011
Discovery of 1,2,4-thiadiazolidine-3,5-dione analogs that exhibit unusual and selective rapid cell death kinetics against acute myelogenous leukemia cells in culture.. 21. 2011
Identification of benzofuran-4,5-diones as novel and selective non-hydroxamic acid, non-peptidomimetic based inhibitors of human peptide deformylase.. 21. 2011
Identification of new inhibitors of protein kinase R guided by statistical modeling.. 21. 2011
Triazoles as γ-secretase modulators.. 21. 2011
A protecting group-free synthesis of deazathiamine: a step toward inhibitor design.. 20. 2010
Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors.. 20. 2010
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.. 20. 2010
Purine derivatives as potent gamma-secretase modulators.. 20. 2010
Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent.. 20. 2010
Fluorinated piperidine acetic acids as gamma-secretase modulators.. 20. 2009
Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability.. 19. 2009
Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.. 19. 2009
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.. 20. 2009
Design, syntheses, and evaluation of Taspase1 inhibitors.. 19. 2009
Aminoparthenolides as novel anti-leukemic agents: Discovery of the NF-kappaB inhibitor, DMAPT (LC-1).. 19. 2009
An efficient chemical approach to bispecific antibodies and antibodies of high valency.. 19. 2009
Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides.. 19. 2009
Multiple catalytic aldolase antibodies suitable for chemical programming.. 19. 2009
Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization.. 19. 2008
SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).. 18. 2008
Mechanism-based inhibitors of MenE, an acyl-CoA synthetase involved in bacterial menaquinone biosynthesis.. 18. 2008
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.. 18. 2008
Design of a fluorescence polarization assay platform for the study of human Hsp70.. 18. 2008
Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).. 18. 2008
A series of novel, potent, and selective histone deacetylase inhibitors.. 16. 2006
Synthesis of a red-shifted fluorescence polarization probe for Hsp90.. 16. 2006
Design and synthesis of potent and subtype-selective PPARalpha agonists.. 16. 2005
Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.. 15. 2005
Synthesis and evaluation of photolabile insulin prodrugs.. 15. 2005
Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.. 15. 2005
Selective PPARgamma modulators with improved pharmacological profiles.. 15. 2005
DNA photocleavage and biological activity of a pyrene dihydrodioxin.. 15. 2005
Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain.. 15. 2005
Thiourea inhibitors of herpesviruses. Part 3: Inhibitors of varicella zoster virus.. 14. 2004
Thiourea inhibitors of herpes viruses. Part 2: N-Benzyl-N'-arylthiourea inhibitors of CMV.. 14. 2004
Synthesis and antitumor evaluation of benzoylphenylurea analogs.. 14. 2004
Synthesis of novel fluorescent probes for the molecular chaperone Hsp90.. 13. 2003
Pyrimido[1,2-b]-1,2,4,5-tetrazin-6-ones as HCMV protease inhibitors: a new class of heterocycles with flavin-like redox properties.. 13. 2003
Thiourea inhibitors of herpes viruses. Part 1: bis-(aryl)thiourea inhibitors of CMV.. 13. 2003
Nodulisporic acid side-chain modifications: access to the 2", 3", 4", and 6" registers.. 13. 2003
Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter.. 12. 2002
Side-chain homologation of nodulisporic acid: synthesis of potent new dienyl derivatives.. 12. 2002
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.. 12. 2002
Fluorescent monitoring of kinase activity in real time: development of a robust fluorescence-based assay for Abl tyrosine kinase activity.. 11. 2001
LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family.. 11. 2001
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1.. 11. 2001
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2.. 11. 2001
Chemical modification of nodulisporic acid A: preliminary structure-activity relationships.. 10. 2000
Synthesis and evaluation of geldanamycin-testosterone hybrids.. 10. 2000
Synthesis and evaluation of geldanamycin-estradiol hybrids.. 9. 1999
Synthesis of gem-difluoro-avermectin derivatives: potent anthelmintic and anticonvulsant agents.. 8. 1998

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