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Structure-activity relationship (SAR) optimization of 6-(indol-2-yl)pyridine-3-sulfonamides: identification of potent, selective, and orally bioavailable small molecules targeting hepatitis C (HCV) NS4B.
Zhang N, Zhang X, Zhu J, Turpoff A, Chen G, Morrill C, Huang S, Lennox W, Kakarla R, Liu R, Li C, Ren H, Almstead N, Venkatraman S, Njoroge FG, Gu Z, Clausen V, Graci J, Jung SP, Zheng Y, Colacino JM, Lahser F, Sheedy J, Mollin A, Weetall M, Nomeir A, Karp GM. Zhang N, et al. Among authors: graci j. J Med Chem. 2014 Mar 13;57(5):2121-35. doi: 10.1021/jm401621g. Epub 2013 Dec 4. J Med Chem. 2014. PMID: 24266880
Discovery of novel HCV inhibitors: synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B.
Zhang X, Zhang N, Chen G, Turpoff A, Ren H, Takasugi J, Morrill C, Zhu J, Li C, Lennox W, Paget S, Liu Y, Almstead N, Njoroge FG, Gu Z, Komatsu T, Clausen V, Espiritu C, Graci J, Colacino J, Lahser F, Risher N, Weetall M, Nomeir A, Karp GM. Zhang X, et al. Among authors: graci j. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3947-53. doi: 10.1016/j.bmcl.2013.04.049. Epub 2013 Apr 30. Bioorg Med Chem Lett. 2013. PMID: 23683597
Discovery of 2-(4-sulfonamidophenyl)-indole 3-carboxamides as potent and selective inhibitors with broad hepatitis C virus genotype activity targeting HCV NS4B.
Zhang N, Turpoff A, Zhang X, Huang S, Liu Y, Almstead N, Njoroge FG, Gu Z, Graci J, Jung SP, Pichardo J, Colacino J, Lahser F, Ingravallo P, Weetall M, Nomeir A, Karp GM. Zhang N, et al. Among authors: graci j. Bioorg Med Chem Lett. 2016 Jan 15;26(2):594-601. doi: 10.1016/j.bmcl.2015.11.065. Epub 2015 Nov 19. Bioorg Med Chem Lett. 2016. PMID: 26652483
Identification of PTC725, an orally bioavailable small molecule that selectively targets the hepatitis C Virus NS4B protein.
Gu Z, Graci JD, Lahser FC, Breslin JJ, Jung SP, Crona JH, McMonagle P, Xia E, Liu S, Karp G, Zhu J, Huang S, Nomeir A, Weetall M, Almstead NG, Peltz SW, Tong X, Ralston R, Colacino JM. Gu Z, et al. Among authors: graci jd. Antimicrob Agents Chemother. 2013 Jul;57(7):3250-61. doi: 10.1128/AAC.00527-13. Epub 2013 Apr 29. Antimicrob Agents Chemother. 2013. PMID: 23629699 Free PMC article.
Identification of benzazole compounds that induce HIV-1 transcription.
Graci JD, Michaels D, Chen G, Schiralli Lester GM, Nodder S, Weetall M, Karp GM, Gu Z, Colacino JM, Henderson AJ. Graci JD, et al. PLoS One. 2017 Jun 28;12(6):e0179100. doi: 10.1371/journal.pone.0179100. eCollection 2017. PLoS One. 2017. PMID: 28658263 Free PMC article.
Targeting of Hematologic Malignancies with PTC299, A Novel Potent Inhibitor of Dihydroorotate Dehydrogenase with Favorable Pharmaceutical Properties.
Cao L, Weetall M, Trotta C, Cintron K, Ma J, Kim MJ, Furia B, Romfo C, Graci JD, Li W, Du J, Sheedy J, Hedrick J, Risher N, Yeh S, Qi H, Arasu T, Hwang S, Lennox W, Kong R, Petruska J, Moon YC, Babiak J, Davis TW, Jacobson A, Almstead NG, Branstrom A, Colacino JM, Peltz SW. Cao L, et al. Among authors: graci jd. Mol Cancer Ther. 2019 Jan;18(1):3-16. doi: 10.1158/1535-7163.MCT-18-0863. Epub 2018 Oct 23. Mol Cancer Ther. 2019. PMID: 30352802 Free PMC article.
Emvododstat, a Potent Dihydroorotate Dehydrogenase Inhibitor, Is Effective in Preclinical Models of Acute Myeloid Leukemia.
Branstrom A, Cao L, Furia B, Trotta C, Santaguida M, Graci JD, Colacino JM, Ray B, Li W, Sheedy J, Mollin A, Yeh S, Kong R, Sheridan R, Baird JD, O'Keefe K, Spiegel R, Goodwin E, Keating S, Weetall M. Branstrom A, et al. Among authors: graci jd. Front Oncol. 2022 Feb 9;12:832816. doi: 10.3389/fonc.2022.832816. eCollection 2022. Front Oncol. 2022. PMID: 35223511 Free PMC article.
35 results