Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 321


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.


Inhibition of adenovirus replication by a trisubstituted piperazin-2-one derivative.

Sanchez-Cespedes J, Moyer CL, Whitby LR, Boger DL, Nemerow GR.

Antiviral Res. 2014 Aug;108:65-73. doi: 10.1016/j.antiviral.2014.05.010. Epub 2014 Jun 4.


α-Ketoheterocycle inhibitors of fatty acid amide hydrolase: exploration of conformational constraints in the acyl side chain.

Duncan KK, Otrubova K, Boger DL.

Bioorg Med Chem. 2014 May 1;22(9):2763-70. doi: 10.1016/j.bmc.2014.03.013. Epub 2014 Mar 18.


Total syntheses of (-)-kopsifoline D and (-)-deoxoapodine: divergent total synthesis via late-stage key strategic bond formation.

Lee K, Boger DL.

J Am Chem Soc. 2014 Feb 26;136(8):3312-7. doi: 10.1021/ja500548e. Epub 2014 Feb 17.


Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase.

Otrubova K, Cravatt BF, Boger DL.

J Med Chem. 2014 Feb 13;57(3):1079-89. doi: 10.1021/jm401820q. Epub 2014 Jan 23.


Insights into the mechanism of streptonigrin-induced protein arginine deiminase inactivation.

Dreyton CJ, Anderson ED, Subramanian V, Boger DL, Thompson PR.

Bioorg Med Chem. 2014 Feb 15;22(4):1362-9. doi: 10.1016/j.bmc.2013.12.064. Epub 2014 Jan 8.


Total syntheses of (-)-pyrimidoblamic acid and P-3A.

Duerfeldt AS, Boger DL.

J Am Chem Soc. 2014 Feb 5;136(5):2119-25. doi: 10.1021/ja412298c. Epub 2014 Jan 21.


Potent Vinblastine C20' Ureas Displaying Additionally Improved Activity Against a Vinblastine-Resistant Cancer Cell Line.

Barker TJ, Duncan KK, Otrubova K, Boger DL.

ACS Med Chem Lett. 2013 Sep 9;4(10). doi: 10.1021/ml400281w.


Transannular Diels-Alder/1,3-dipolar cycloaddition cascade of 1,3,4-oxadiazoles: total synthesis of a unique set of vinblastine analogues.

Campbell EL, Skepper CK, Sankar K, Duncan KK, Boger DL.

Org Lett. 2013 Oct 18;15(20):5306-9. doi: 10.1021/ol402549n. Epub 2013 Oct 2.


A fundamental relationship between hydrophobic properties and biological activity for the duocarmycin class of DNA-alkylating antitumor drugs: hydrophobic-binding-driven bonding.

Wolfe AL, Duncan KK, Lajiness JP, Zhu K, Duerfeldt AS, Boger DL.

J Med Chem. 2013 Sep 12;56(17):6845-57. doi: 10.1021/jm400665c. Epub 2013 Aug 29.


NMR-assisted computational studies of peptidomimetic inhibitors bound in the hydrophobic pocket of HIV-1 glycoprotein 41.

Gochin M, Whitby LR, Phillips AH, Boger DL.

J Comput Aided Mol Des. 2013 Jul;27(7):569-82. doi: 10.1007/s10822-013-9662-6. Epub 2013 Jul 27.


Investigation into the functional impact of the vancomycin C-ring aryl chloride.

Pinchman JR, Boger DL.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4817-9. doi: 10.1016/j.bmcl.2013.06.080. Epub 2013 Jul 4.

Supplemental Content

Loading ...
Support Center