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116 results

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Page 1
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Gong H, Weinstein DS, Lu Z, Duan JJ, Stachura S, Haque L, Karmakar A, Hemagiri H, Raut DK, Gupta AK, Khan J, Camac D, Sack JS, Pudzianowski A, Wu DR, Yarde M, Shen DR, Borowski V, Xie JH, Sun H, D'Arienzo C, Dabros M, Galella MA, Wang F, Weigelt CA, Zhao Q, Foster W, Somerville JE, Salter-Cid LM, Barrish JC, Carter PH, Dhar TGM. Gong H, et al. Among authors: sack js. Bioorg Med Chem Lett. 2018 Jan 15;28(2):85-93. doi: 10.1016/j.bmcl.2017.12.006. Epub 2017 Dec 5. Bioorg Med Chem Lett. 2018. PMID: 29233651
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.
Cherney RJ, Cornelius LAM, Srivastava A, Weigelt CA, Marcoux D, Duan JJ, Shi Q, Batt DG, Liu Q, Yip S, Wu DR, Ruzanov M, Sack J, Khan J, Wang J, Yarde M, Cvijic ME, Mathur A, Li S, Shuster D, Khandelwal P, Borowski V, Xie J, Obermeier M, Fura A, Stefanski K, Cornelius G, Tino JA, Macor JE, Salter-Cid L, Denton R, Zhao Q, Carter PH, Dhar TGM. Cherney RJ, et al. ACS Med Chem Lett. 2020 Mar 31;11(6):1221-1227. doi: 10.1021/acsmedchemlett.0c00063. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551004 Free PMC article.
Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Shi Q, Xiao Z, Yang MG, Marcoux D, Cherney RJ, Yip S, Li P, Wu DR, Weigelt CA, Sack J, Khan J, Ruzanov M, Wang J, Yarde M, Ellen Cvijic M, Li S, Shuster DJ, Xie J, Sherry T, Obermeier M, Fura A, Stefanski K, Cornelius G, Chacko S, Shu YZ, Khandelwal P, Hynes J Jr, Tino JA, Salter-Cid L, Denton R, Zhao Q, Dhar TGM. Shi Q, et al. Bioorg Med Chem Lett. 2020 Dec 1;30(23):127521. doi: 10.1016/j.bmcl.2020.127521. Epub 2020 Aug 31. Bioorg Med Chem Lett. 2020. PMID: 32882417
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.
Duan JJ, Lu Z, Jiang B, Yang BV, Doweyko LM, Nirschl DS, Haque LE, Lin S, Brown G, Hynes J Jr, Tokarski JS, Sack JS, Khan J, Lippy JS, Zhang RF, Pitt S, Shen G, Pitts WJ, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, McKinnon M, Fura A, Schieven GL, Wrobleski ST. Duan JJ, et al. Among authors: sack js. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5721-5726. doi: 10.1016/j.bmcl.2014.10.061. Epub 2014 Oct 24. Bioorg Med Chem Lett. 2014. PMID: 25453808
Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3Kδ inhibitors.
Bhide RS, Neels J, Qin LY, Ruan Z, Stachura S, Weigelt C, Sack JS, Stefanski K, Gu X, Xie JH, Goldstine CB, Skala S, Pedicord DL, Ruepp S, Dhar TG, Carter PH, Salter-Cid LM, Poss MA, Davies P. Bhide RS, et al. Among authors: sack js. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4256-60. doi: 10.1016/j.bmcl.2016.07.047. Epub 2016 Jul 21. Bioorg Med Chem Lett. 2016. PMID: 27476421
Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors.
Qin LY, Ruan Z, Cherney RJ, Dhar TGM, Neels J, Weigelt CA, Sack JS, Srivastava AS, Cornelius LAM, Tino JA, Stefanski K, Gu X, Xie J, Susulic V, Yang X, Yarde-Chinn M, Skala S, Bosnius R, Goldstein C, Davies P, Ruepp S, Salter-Cid L, Bhide RS, Poss MA. Qin LY, et al. Among authors: sack js. Bioorg Med Chem Lett. 2017 Feb 15;27(4):855-861. doi: 10.1016/j.bmcl.2017.01.016. Epub 2017 Jan 10. Bioorg Med Chem Lett. 2017. PMID: 28108251
Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.
Hynes J Jr, Wu H, Kempson J, Duan JJ, Lu Z, Jiang B, Stachura S, Tokarski JS, Sack JS, Khan JA, Lippy JS, Zhang RF, Pitt S, Shen G, Gillooly K, McIntyre K, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, Fura A, Schieven GL, Pitts WJ, Wrobleski ST. Hynes J Jr, et al. Among authors: sack js. Bioorg Med Chem Lett. 2017 Jul 15;27(14):3101-3106. doi: 10.1016/j.bmcl.2017.05.043. Epub 2017 May 15. Bioorg Med Chem Lett. 2017. PMID: 28539220
Discovery of highly potent, selective, covalent inhibitors of JAK3.
Kempson J, Ovalle D, Guo J, Wrobleski ST, Lin S, Spergel SH, Duan JJ, Jiang B, Lu Z, Das J, Yang BV, Hynes J Jr, Wu H, Tokarski J, Sack JS, Khan J, Schieven G, Blatt Y, Chaudhry C, Salter-Cid LM, Fura A, Barrish JC, Carter PH, Pitts WJ. Kempson J, et al. Among authors: sack js. Bioorg Med Chem Lett. 2017 Oct 15;27(20):4622-4625. doi: 10.1016/j.bmcl.2017.09.023. Epub 2017 Sep 11. Bioorg Med Chem Lett. 2017. PMID: 28927786
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.
Duan JJ, Lu Z, Jiang B, Stachura S, Weigelt CA, Sack JS, Khan J, Ruzanov M, Galella MA, Wu DR, Yarde M, Shen DR, Shuster DJ, Borowski V, Xie JH, Zhang L, Vanteru S, Gupta AK, Mathur A, Zhao Q, Foster W, Salter-Cid LM, Carter PH, Dhar TGM. Duan JJ, et al. Among authors: sack js. ACS Med Chem Lett. 2019 Feb 26;10(3):367-373. doi: 10.1021/acsmedchemlett.9b00010. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891142 Free PMC article.
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists.
Lu Z, Duan JJ, Xiao H, Neels J, Wu DR, Weigelt CA, Sack JS, Khan J, Ruzanov M, An Y, Yarde M, Karmakar A, Vishwakrishnan S, Baratam V, Shankarappa H, Vanteru S, Babu V, Basha M, Kumar Gupta A, Kumaravel S, Mathur A, Zhao Q, Salter-Cid LM, Carter PH, Murali Dhar TG. Lu Z, et al. Among authors: sack js. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2265-2269. doi: 10.1016/j.bmcl.2019.06.036. Epub 2019 Jun 20. Bioorg Med Chem Lett. 2019. PMID: 31257087
116 results