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Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions.

Tosh DK, Paoletta S, Phan K, Gao ZG, Jacobson KA.

ACS Med Chem Lett. 2012 Jul 12;3(7):596-601. Epub 2012 Jun 11.


Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.

Tosh DK, Deflorian F, Phan K, Gao ZG, Wan TC, Gizewski E, Auchampach JA, Jacobson KA.

J Med Chem. 2012 May 24;55(10):4847-60. doi: 10.1021/jm300396n. Epub 2012 May 16.


Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.

Tosh DK, Chinn M, Ivanov AA, Klutz AM, Gao ZG, Jacobson KA.

J Med Chem. 2009 Dec 10;52(23):7580-92. doi: 10.1021/jm900426g.


(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.

Tchilibon S, Joshi BV, Kim SK, Duong HT, Gao ZG, Jacobson KA.

J Med Chem. 2005 Mar 24;48(6):1745-58.


Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.

Melman A, Wang B, Joshi BV, Gao ZG, Castro Sd, Heller CL, Kim SK, Jeong LS, Jacobson KA.

Bioorg Med Chem. 2008 Sep 15;16(18):8546-56. doi: 10.1016/j.bmc.2008.08.007. Epub 2008 Aug 7.


Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.

Melman A, Gao ZG, Kumar D, Wan TC, Gizewski E, Auchampach JA, Jacobson KA.

Bioorg Med Chem Lett. 2008 May 1;18(9):2813-9. doi: 10.1016/j.bmcl.2008.04.001. Epub 2008 Apr 4.


Click modification in the N6 region of A3 adenosine receptor-selective carbocyclic nucleosides for dendrimeric tethering that preserves pharmacophore recognition.

Tosh DK, Phan K, Deflorian F, Wei Q, Yoo LS, Gao ZG, Jacobson KA.

Bioconjug Chem. 2012 Feb 15;23(2):232-47. doi: 10.1021/bc200526c. Epub 2012 Jan 11.


Extended N(6) substitution of rigid C2-arylethynyl nucleosides for exploring the role of extracellular loops in ligand recognition at the A3 adenosine receptor.

Tosh DK, Paoletta S, Chen Z, Moss SM, Gao ZG, Salvemini D, Jacobson KA.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3302-6. doi: 10.1016/j.bmcl.2014.06.006. Epub 2014 Jun 11.


Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.

Gao ZG, Kim SK, Biadatti T, Chen W, Lee K, Barak D, Kim SG, Johnson CR, Jacobson KA.

J Med Chem. 2002 Sep 26;45(20):4471-84.


Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.

Tosh DK, Phan K, Deflorian F, Wei Q, Gao ZG, Jacobson KA.

ACS Med Chem Lett. 2011 Aug 11;2(8):626-631.


Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A₂A and A₃ adenosine receptor ligands.

Hou X, Majik MS, Kim K, Pyee Y, Lee Y, Alexander V, Chung HJ, Lee HW, Chandra G, Lee JH, Park SG, Choi WJ, Kim HO, Phan K, Gao ZG, Jacobson KA, Choi S, Lee SK, Jeong LS.

J Med Chem. 2012 Jan 12;55(1):342-56. doi: 10.1021/jm201229j. Epub 2011 Dec 28.


Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.

Jacobson KA, Ji X, Li AH, Melman N, Siddiqui MA, Shin KJ, Marquez VE, Ravi RG.

J Med Chem. 2000 Jun 1;43(11):2196-203.


Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor.

Jeong LS, Lee HW, Jacobson KA, Kim HO, Shin DH, Lee JA, Gao ZG, Lu C, Duong HT, Gunaga P, Lee SK, Jin DZ, Chun MW, Moon HR.

J Med Chem. 2006 Jan 12;49(1):273-81.


Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.

Pal S, Choi WJ, Choe SA, Heller CL, Gao ZG, Chinn M, Jacobson KA, Hou X, Lee SK, Kim HO, Jeong LS.

Bioorg Med Chem. 2009 May 15;17(10):3733-8. doi: 10.1016/j.bmc.2009.03.034. Epub 2009 Mar 25.


N6-Substituted adenosine derivatives: selectivity, efficacy, and species differences at A3 adenosine receptors.

Gao ZG, Blaustein JB, Gross AS, Melman N, Jacobson KA.

Biochem Pharmacol. 2003 May 15;65(10):1675-84.


In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.

Tosh DK, Finley A, Paoletta S, Moss SM, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA.

J Med Chem. 2014 Dec 11;57(23):9901-14. doi: 10.1021/jm501021n. Epub 2014 Nov 25.


Exploring distal regions of the A3 adenosine receptor binding site: sterically constrained N6-(2-phenylethyl)adenosine derivatives as potent ligands.

Tchilibon S, Kim SK, Gao ZG, Harris BA, Blaustein JB, Gross AS, Duong HT, Melman N, Jacobson KA.

Bioorg Med Chem. 2004 May 1;12(9):2021-34.


2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists.

Kim HS, Ohno M, Xu B, Kim HO, Choi Y, Ji XD, Maddileti S, Marquez VE, Harden TK, Jacobson KA.

J Med Chem. 2003 Nov 6;46(23):4974-87.


Partial agonists for A(3) adenosine receptors.

Gao ZG, Jacobson KA.

Curr Top Med Chem. 2004;4(8):855-62. Review.


5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.

Cappellacci L, Franchetti P, Vita P, Petrelli R, Lavecchia A, Costa B, Spinetti F, Martini C, Klotz KN, Grifantini M.

Bioorg Med Chem. 2008 Jan 1;16(1):336-53. Epub 2007 Sep 22.


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