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C1-CBP-vancomycin: Impact of a Vancomycin C-Terminus Trimethylammonium Cation on Pharmacological Properties and Insights into Its Newly Introduced Mechanism of Action.

Wu ZC, Isley NA, Okano A, Weiss WJ, Boger DL.

J Org Chem. 2020 Feb 7;85(3):1365-1375. doi: 10.1021/acs.joc.9b02314. Epub 2019 Oct 31.


Total Synthesis and Stereochemical Assignment of Streptide.

Isley NA, Endo Y, Wu ZC, Covington BC, Bushin LB, Seyedsayamdost MR, Boger DL.

J Am Chem Soc. 2019 Oct 30;141(43):17361-17369. doi: 10.1021/jacs.9b09067. Epub 2019 Oct 17.


SAR studies of 4-acyl-1,6-dialkylpiperazin-2-one arenavirus cell entry inhibitors.

Plewe MB, Whitby LR, Naik S, Brown ER, Sokolova NV, Gantla VR, York J, Nunberg JH, Zhang L, Kalveram B, Freiberg AN, Boger DL, Henkel G, McCormack K.

Bioorg Med Chem Lett. 2019 Nov 15;29(22):126620. doi: 10.1016/j.bmcl.2019.08.024. Epub 2019 Aug 24.


Synthesis, Characterization, and Cycloaddition Reactivity of a Monocyclic Aromatic 1,2,3,5-Tetrazine.

Wu ZC, Boger DL.

J Am Chem Soc. 2019 Oct 16;141(41):16388-16397. doi: 10.1021/jacs.9b07744. Epub 2019 Oct 2.


Triarylaminium Radical Cation Promoted Coupling of Catharanthine with Vindoline: Diastereospecific Synthesis of Anhydrovinblastine and Reaction Scope.

Boon BA, Boger DL.

J Am Chem Soc. 2019 Sep 11;141(36):14349-14355. doi: 10.1021/jacs.9b06968. Epub 2019 Sep 3.


Resveratrol trimer enhances gene delivery to hematopoietic stem cells by reducing antiviral restriction at endosomes.

Ozog S, Timberlake ND, Hermann K, Garijo O, Haworth KG, Shi G, Glinkerman CM, Schefter LE, D'Souza S, Simpson E, Sghia-Hughes G, Carillo RR, Boger DL, Kiem HP, Slukvin I, Ryu BY, Sorrentino BP, Adair JE, Snyder SA, Compton AA, Torbett BE.

Blood. 2019 Oct 17;134(16):1298-1311. doi: 10.1182/blood.2019000040.


Exploration of the site-specific nature and generalizability of a trimethylammonium salt modification on vancomycin: A-ring derivatives.

Wu ZC, Boger DL.

Tetrahedron. 2019 Jun 14;75(24):3160-3165. doi: 10.1016/j.tet.2019.02.008. Epub 2019 Feb 4.


Inverse Electron Demand Diels-Alder Reactions of Heterocyclic Azadienes, 1-Aza-1,3-Butadienes, Cyclopropenone Ketals, and Related Systems. A Retrospective.

Zhang J, Shukla V, Boger DL.

J Org Chem. 2019 Aug 2;84(15):9397-9445. doi: 10.1021/acs.joc.9b00834. Epub 2019 May 23.


Ultra-potent vinblastine analogues improve on-target activity of the parent microtubulin-targeting compound.

Radakovic A, Boger DL.

Bioorg Med Chem Lett. 2019 Jun 1;29(11):1370-1374. doi: 10.1016/j.bmcl.2019.03.036. Epub 2019 Mar 26.


N-Acyl pyrazoles: Effective and tunable inhibitors of serine hydrolases.

Otrubova K, Chatterjee S, Ghimire S, Cravatt BF, Boger DL.

Bioorg Med Chem. 2019 Apr 15;27(8):1693-1703. doi: 10.1016/j.bmc.2019.03.020. Epub 2019 Mar 11.


Structural Basis of TLR2/TLR1 Activation by the Synthetic Agonist Diprovocim.

Su L, Wang Y, Wang J, Mifune Y, Morin MD, Jones BT, Moresco EMY, Boger DL, Beutler B, Zhang H.

J Med Chem. 2019 Mar 28;62(6):2938-2949. doi: 10.1021/acs.jmedchem.8b01583. Epub 2019 Mar 13.


Diprovocims: A New and Exceptionally Potent Class of Toll-like Receptor Agonists.

Morin MD, Wang Y, Jones BT, Mifune Y, Su L, Shi H, Moresco EMY, Zhang H, Beutler B, Boger DL.

J Am Chem Soc. 2018 Oct 31;140(43):14440-14454. doi: 10.1021/jacs.8b09223. Epub 2018 Oct 16.


Adjuvant effect of the novel TLR1/TLR2 agonist Diprovocim synergizes with anti-PD-L1 to eliminate melanoma in mice.

Wang Y, Su L, Morin MD, Jones BT, Mifune Y, Shi H, Wang KW, Zhan X, Liu A, Wang J, Li X, Tang M, Ludwig S, Hildebrand S, Zhou K, Siegwart DJ, Moresco EMY, Zhang H, Boger DL, Beutler B.

Proc Natl Acad Sci U S A. 2018 Sep 11;115(37):E8698-E8706. doi: 10.1073/pnas.1809232115. Epub 2018 Aug 27.


N-Terminus Alkylation of Vancomycin: Ligand Binding Affinity, Antimicrobial Activity, and Site-Specific Nature of Quaternary Trimethylammonium Salt Modification.

Wu ZC, Isley NA, Boger DL.

ACS Infect Dis. 2018 Oct 12;4(10):1468-1474. doi: 10.1021/acsinfecdis.8b00152. Epub 2018 Aug 8.


Synthesis, Characterization, and Rapid Cycloadditions of 5-Nitro-1,2,3-triazine.

Glinkerman CM, Boger DL.

Org Lett. 2018 May 4;20(9):2628-2631. doi: 10.1021/acs.orglett.8b00825. Epub 2018 Apr 16.


Duocarmycin SA, a potent antitumor antibiotic, sensitizes glioblastoma cells to proton radiation.

Boyle KE, Boger DL, Wroe A, Vazquez M.

Bioorg Med Chem Lett. 2018 Sep 1;28(16):2688-2692. doi: 10.1016/j.bmcl.2018.04.008. Epub 2018 Apr 4.


High expression of class III β-tubulin has no impact on functional cancer cell growth inhibition of a series of key vinblastine analogs.

Radakovic A, Boger DL.

Bioorg Med Chem Lett. 2018 Mar 1;28(5):863-865. doi: 10.1016/j.bmcl.2018.02.006. Epub 2018 Feb 6.


The Difference a Single Atom Can Make: Synthesis and Design at the Chemistry-Biology Interface.

Boger DL.

J Org Chem. 2017 Dec 1;82(23):11961-11980. doi: 10.1021/acs.joc.7b02088. Epub 2017 Oct 13.


Vinblastine 20' Amides: Synthetic Analogues That Maintain or Improve Potency and Simultaneously Overcome Pgp-Derived Efflux and Resistance.

Lukesh JC 3rd, Carney DW, Dong H, Cross RM, Shukla V, Duncan KK, Yang S, Brody DM, Brütsch MM, Radakovic A, Boger DL.

J Med Chem. 2017 Sep 14;60(17):7591-7604. doi: 10.1021/acs.jmedchem.7b00958. Epub 2017 Aug 31.


Direct Synthesis of β-Aminoenals through Reaction of 1,2,3-Triazine with Secondary Amines.

Quiñones RE, Glinkerman CM, Zhu K, Boger DL.

Org Lett. 2017 Jul 7;19(13):3568-3571. doi: 10.1021/acs.orglett.7b01543. Epub 2017 Jun 28.


Peripheral modifications of [Ψ[CH2NH]Tpg4]vancomycin with added synergistic mechanisms of action provide durable and potent antibiotics.

Okano A, Isley NA, Boger DL.

Proc Natl Acad Sci U S A. 2017 Jun 27;114(26):E5052-E5061. doi: 10.1073/pnas.1704125114. Epub 2017 May 30.


Key analogs of a uniquely potent synthetic vinblastine that contain modifications of the C20' ethyl substituent.

Allemann O, Cross RM, Brütsch MM, Radakovic A, Boger DL.

Bioorg Med Chem Lett. 2017 Jul 15;27(14):3055-3059. doi: 10.1016/j.bmcl.2017.05.058. Epub 2017 May 18.


Design of Benzoxathiazin-3-one 1,1-Dioxides as a New Class of Irreversible Serine Hydrolase Inhibitors: Discovery of a Uniquely Selective PNPLA4 Inhibitor.

Kornahrens AF, Cognetta AB 3rd, Brody DM, Matthews ML, Cravatt BF, Boger DL.

J Am Chem Soc. 2017 May 24;139(20):7052-7061. doi: 10.1021/jacs.7b02985. Epub 2017 May 12.


Total Syntheses of Vancomycin-Related Glycopeptide Antibiotics and Key Analogues.

Okano A, Isley NA, Boger DL.

Chem Rev. 2017 Sep 27;117(18):11952-11993. doi: 10.1021/acs.chemrev.6b00820. Epub 2017 Apr 24. Review.


Total synthesis of a key series of vinblastines modified at C4 that define the importance and surprising trends in activity.

Yang S, Sankar K, Skepper CK, Barker TJ, Lukesh JC 3rd, Brody DM, Brütsch MM, Boger DL.

Chem Sci. 2017 Feb 1;8(2):1560-1569. doi: 10.1039/C6SC04146A. Epub 2016 Nov 3.


Catalysis of Heterocyclic Azadiene Cycloaddition Reactions by Solvent Hydrogen Bonding: Concise Total Synthesis of Methoxatin.

Glinkerman CM, Boger DL.

J Am Chem Soc. 2016 Sep 28;138(38):12408-13. doi: 10.1021/jacs.6b05438. Epub 2016 Sep 14.


Ultrapotent vinblastines in which added molecular complexity further disrupts the target tubulin dimer-dimer interface.

Carney DW, Lukesh JC 3rd, Brody DM, Brütsch MM, Boger DL.

Proc Natl Acad Sci U S A. 2016 Aug 30;113(35):9691-8. doi: 10.1073/pnas.1611405113. Epub 2016 Aug 10.


Synthesis of a Potent Vinblastine: Rationally Designed Added Benign Complexity.

Allemann O, Brutsch M, Lukesh JC 3rd, Brody DM, Boger DL.

J Am Chem Soc. 2016 Jul 13;138(27):8376-9. doi: 10.1021/jacs.6b04330. Epub 2016 Jul 1.


Synthesis and evaluation of duocarmycin SA analogs incorporating the methyl 1,2,8,8a-tetrahydrocyclopropa[c]imidazolo[4,5-e]indol-4-one-6-carboxylate (CImI) alkylation subunit.

Chanda PB, Boyle KE, Brody DM, Shukla V, Boger DL.

Bioorg Med Chem. 2016 Oct 15;24(20):4779-4786. doi: 10.1016/j.bmc.2016.04.050. Epub 2016 Apr 26.


Small-Molecule Fusion Inhibitors Bind the pH-Sensing Stable Signal Peptide-GP2 Subunit Interface of the Lassa Virus Envelope Glycoprotein.

Shankar S, Whitby LR, Casquilho-Gray HE, York J, Boger DL, Nunberg JH.

J Virol. 2016 Jul 11;90(15):6799-807. doi: 10.1128/JVI.00597-16. Print 2016 Aug 1.


FAAH inhibitor OL-135 disrupts contextual, but not auditory, fear conditioning in rats.

Burman MA, Szolusha K, Bind R, Kerney K, Boger DL, Bilsky EJ.

Behav Brain Res. 2016 Jul 15;308:1-5. doi: 10.1016/j.bbr.2016.04.014. Epub 2016 Apr 13.


Discovery and Structure-Activity Relationships of the Neoseptins: A New Class of Toll-like Receptor-4 (TLR4) Agonists.

Morin MD, Wang Y, Jones BT, Su L, Surakattula MM, Berger M, Huang H, Beutler EK, Zhang H, Beutler B, Boger DL.

J Med Chem. 2016 May 26;59(10):4812-30. doi: 10.1021/acs.jmedchem.6b00177. Epub 2016 Apr 25.


TLR4/MD-2 activation by a synthetic agonist with no similarity to LPS.

Wang Y, Su L, Morin MD, Jones BT, Whitby LR, Surakattula MM, Huang H, Shi H, Choi JH, Wang KW, Moresco EM, Berger M, Zhan X, Zhang H, Boger DL, Beutler B.

Proc Natl Acad Sci U S A. 2016 Feb 16;113(7):E884-93. doi: 10.1073/pnas.1525639113. Epub 2016 Feb 1. Erratum in: Proc Natl Acad Sci U S A. 2016 Apr 5;113(14 ):E2096.


Tandem Intramolecular Diels-Alder/1,3-Dipolar Cycloaddition Cascade of 1,3,4-Oxadiazoles: Initial Scope and Applications.

Sears JE, Boger DL.

Acc Chem Res. 2016 Feb 16;49(2):241-51. doi: 10.1021/acs.accounts.5b00510. Epub 2016 Jan 27.


Comprehensive Analysis of Structure-Activity Relationships of α-Ketoheterocycles as sn-1-Diacylglycerol Lipase α Inhibitors.

Janssen FJ, Baggelaar MP, Hummel JJ, Overkleeft HS, Cravatt BF, Boger DL, van der Stelt M.

J Med Chem. 2015 Dec 24;58(24):9742-53. doi: 10.1021/acs.jmedchem.5b01627. Epub 2015 Dec 2.


ORGANIC SYNTHESIS. When sugar is not so sweet.

Boger DL.

Science. 2015 Oct 16;350(6258):275-6. doi: 10.1126/science.aad3298. No abstract available.



Boger DL.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4713. doi: 10.1016/j.bmcl.2015.08.082. Epub 2015 Sep 1. No abstract available.


Cycloadditions of 1,2,3-Triazines Bearing C5-Electron Donating Substituents: Robust Pyrimidine Synthesis.

Glinkerman CM, Boger DL.

Org Lett. 2015 Aug 21;17(16):4002-5. doi: 10.1021/acs.orglett.5b01870. Epub 2015 Jul 14.


Total synthesis of (-)-kopsinine and ent-(+)-kopsinine.

Lee K, Boger DL.

Tetrahedron. 2015 Jun 3;71(22):3741-3746.


A five-membered lactone prodrug of CBI-based analogs of the duocarmycins.

Uematsu M, Brody DM, Boger DL.

Tetrahedron Lett. 2015 Jun 3;56(23):3101-3104.


Target-based screen against a periplasmic serine protease that regulates intrabacterial pH homeostasis in Mycobacterium tuberculosis.

Zhao N, Darby CM, Small J, Bachovchin DA, Jiang X, Burns-Huang KE, Botella H, Ehrt S, Boger DL, Anderson ED, Cravatt BF, Speers AE, Fernandez-Vega V, Hodder PS, Eberhart C, Rosen H, Spicer TP, Nathan CF.

ACS Chem Biol. 2015 Feb 20;10(2):364-71. doi: 10.1021/cb500746z. Epub 2014 Dec 5.


Asymmetric synthesis of a CBI-based cyclic N-acyl O-amino phenol duocarmycin prodrug.

Uematsu M, Boger DL.

J Org Chem. 2014 Oct 17;79(20):9699-703. doi: 10.1021/jo501839x. Epub 2014 Oct 3.


Cycloadditions of noncomplementary substituted 1,2,3-triazines.

Anderson ED, Duerfeldt AS, Zhu K, Glinkerman CM, Boger DL.

Org Lett. 2014 Oct 3;16(19):5084-7. doi: 10.1021/ol502436n. Epub 2014 Sep 15.


Discovery libraries targeting the major enzyme classes: the serine hydrolases.

Otrubova K, Srinivasan V, Boger DL.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3807-13. doi: 10.1016/j.bmcl.2014.06.063. Epub 2014 Jun 27.


Enzymatic glycosylation of vancomycin aglycon: completion of a total synthesis of vancomycin and N- and C-terminus substituent effects of the aglycon substrate.

Nakayama A, Okano A, Feng Y, Collins JC, Collins KC, Walsh CT, Boger DL.

Org Lett. 2014 Jul 3;16(13):3572-5. doi: 10.1021/ol501568t. Epub 2014 Jun 23.

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