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Page 1
Discovery of Azaindole Ureas as a Novel Class of Bacterial Gyrase B Inhibitors.
Zhang J, Yang Q, Cross JB, Romero JA, Poutsiaka KM, Epie F, Bevan D, Wang B, Zhang Y, Chavan A, Zhang X, Moy T, Daniel A, Nguyen K, Chamberlain B, Carter N, Shotwell J, Silverman J, Metcalf CA 3rd, Ryan D, Lippa B, Dolle RE. Zhang J, et al. Among authors: romero ja. J Med Chem. 2015 Nov 12;58(21):8503-12. doi: 10.1021/acs.jmedchem.5b00961. Epub 2015 Oct 22. J Med Chem. 2015. PMID: 26460684
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
Zhang J, Yang Q, Romero JA, Cross J, Wang B, Poutsiaka KM, Epie F, Bevan D, Wu Y, Moy T, Daniel A, Chamberlain B, Carter N, Shotwell J, Arya A, Kumar V, Silverman J, Nguyen K, Metcalf CA 3rd, Ryan D, Lippa B, Dolle RE. Zhang J, et al. Among authors: romero ja. ACS Med Chem Lett. 2015 Sep 8;6(10):1080-5. doi: 10.1021/acsmedchemlett.5b00266. eCollection 2015 Oct 8. ACS Med Chem Lett. 2015. PMID: 26487916 Free PMC article.
Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design.
Cross JB, Zhang J, Yang Q, Mesleh MF, Romero JA, Wang B, Bevan D, Poutsiaka KM, Epie F, Moy T, Daniel A, Shotwell J, Chamberlain B, Carter N, Andersen O, Barker J, Ryan MD, Metcalf CA 3rd, Silverman J, Nguyen K, Lippa B, Dolle RE. Cross JB, et al. Among authors: romero ja. ACS Med Chem Lett. 2016 Feb 16;7(4):374-8. doi: 10.1021/acsmedchemlett.5b00368. eCollection 2016 Apr 14. ACS Med Chem Lett. 2016. PMID: 27096044 Free PMC article.
Structure-based discovery of LpxC inhibitors.
Zhang J, Chan A, Lippa B, Cross JB, Liu C, Yin N, Romero JA, Lawrence J, Heney R, Herradura P, Goss J, Clark C, Abel C, Zhang Y, Poutsiaka KM, Epie F, Conrad M, Mahamoon A, Nguyen K, Chavan A, Clark E, Li TC, Cheng RK, Wood M, Andersen OA, Brooks M, Kwong J, Barker J, Parr IB, Gu Y, Ryan MD, Coleman S, Metcalf CA 3rd. Zhang J, et al. Among authors: romero ja. Bioorg Med Chem Lett. 2017 Apr 15;27(8):1670-1680. doi: 10.1016/j.bmcl.2017.03.006. Epub 2017 Mar 6. Bioorg Med Chem Lett. 2017. PMID: 28302397
Discovery of indole inhibitors of chemokine receptor 9 (CCR9).
Pandya BA, Baber C, Chan A, Chamberlain B, Chandonnet H, Goss J, Hopper T, Lippa B, Poutsiaka K, Romero J, Stucka S, Varoglu M, Zhang J, Zhang X. Pandya BA, et al. Bioorg Med Chem Lett. 2016 Jul 15;26(14):3322-3325. doi: 10.1016/j.bmcl.2016.05.043. Epub 2016 May 14. Bioorg Med Chem Lett. 2016. PMID: 27256913
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
Durand-Réville TF, Comita-Prevoir J, Zhang J, Wu X, May-Dracka TL, Romero JAC, Wu F, Chen A, Shapiro AB, Carter NM, McLeod SM, Giacobbe RA, Verheijen JC, Lahiri SD, Sacco MD, Chen Y, O'Donnell JP, Miller AA, Mueller JP, Tommasi RA. Durand-Réville TF, et al. J Med Chem. 2020 Nov 12;63(21):12511-12525. doi: 10.1021/acs.jmedchem.0c00579. Epub 2020 Jul 24. J Med Chem. 2020. PMID: 32658473 Free PMC article.
Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease.
Zhang J, Romero J, Chan A, Goss J, Stucka S, Cross J, Chamberlain B, Varoglu M, Chandonnet H, Ryan D, Lippa B. Zhang J, et al. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3661-4. doi: 10.1016/j.bmcl.2015.06.046. Epub 2015 Jun 18. Bioorg Med Chem Lett. 2015. PMID: 26117562
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.
Huang WS, Metcalf CA, Sundaramoorthi R, Wang Y, Zou D, Thomas RM, Zhu X, Cai L, Wen D, Liu S, Romero J, Qi J, Chen I, Banda G, Lentini SP, Das S, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Zhou T, Commodore L, Narasimhan NI, Mohemmad QK, Iuliucci J, Rivera VM, Dalgarno DC, Sawyer TK, Clackson T, Shakespeare WC. Huang WS, et al. J Med Chem. 2010 Jun 24;53(12):4701-19. doi: 10.1021/jm100395q. J Med Chem. 2010. PMID: 20513156
In-silico guided discovery of novel CCR9 antagonists.
Zhang X, Cross JB, Romero J, Heifetz A, Humphries E, Hall K, Wu Y, Stucka S, Zhang J, Chandonnet H, Lippa B, Ryan MD, Baber JC. Zhang X, et al. J Comput Aided Mol Des. 2018 Apr;32(4):573-582. doi: 10.1007/s10822-018-0113-2. Epub 2018 Mar 26. J Comput Aided Mol Des. 2018. PMID: 29582229
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Thomas M, Huang WS, Wen D, Zhu X, Wang Y, Metcalf CA, Liu S, Chen I, Romero J, Zou D, Sundaramoorthi R, Li F, Qi J, Cai L, Zhou T, Commodore L, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Iuliucci J, Rivera VM, Sawyer TK, Dalgarno DC, Clackson T, Shakespeare WC. Thomas M, et al. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3743-8. doi: 10.1016/j.bmcl.2011.04.060. Epub 2011 Apr 22. Bioorg Med Chem Lett. 2011. PMID: 21561767
146 results