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Page 1
Discovery of A-910, a Highly Potent and Orally Bioavailable Dual MerTK/Axl-Selective Tyrosine Kinase Inhibitor.
Yu Y, Jang M, Miyashiro J, Clark RF, Zhu GD, Gong J, Dai Y, Frey RR, Penning TD, Kim H, Lee HK, Kim JK, Ryu KM, Park SJ, Yoon T, Li T, Kurnick MD, Kapecki NJ, Li L, Gorman JV, Montgomery DA, Manaves V, Bromberg KD, Doktor SZ, Thakur A, Wang J, Smith HA, Buchanan FG, Ferguson DC, Torrent M, Jakob CG, Qiu W, Upadhyay AK, Martin RL, Lai A, Michaelides MR. Yu Y, et al. Among authors: clark rf. J Med Chem. 2024 Oct 10;67(19):17000-17032. doi: 10.1021/acs.jmedchem.4c01450. Epub 2024 Sep 16. J Med Chem. 2024. PMID: 39283694
Discovery of spirohydantoins as selective, orally bioavailable inhibitors of p300/CBP histone acetyltransferases.
Ji Z, Clark RF, Bhat V, Matthew Hansen T, Lasko LM, Bromberg KD, Manaves V, Algire M, Martin R, Qiu W, Torrent M, Jakob CG, Liu H, Cole PA, Marmorstein R, Kesicki EA, Lai A, Michaelides MR. Ji Z, et al. Among authors: clark rf. Bioorg Med Chem Lett. 2021 May 1;39:127854. doi: 10.1016/j.bmcl.2021.127854. Epub 2021 Feb 23. Bioorg Med Chem Lett. 2021. PMID: 33631370 Free PMC article.
SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Curtin ML, Pliushchev MA, Li HQ, Torrent M, Dietrich JD, Jakob CG, Zhu H, Zhao H, Wang Y, Ji Z, Clark RF, Sarris KA, Selvaraju S, Shaw B, Algire MA, He Y, Richardson PL, Sweis RF, Sun C, Chiang GG, Michaelides MR. Curtin ML, et al. Among authors: clark rf. Bioorg Med Chem Lett. 2017 Apr 1;27(7):1576-1583. doi: 10.1016/j.bmcl.2017.02.030. Epub 2017 Feb 20. Bioorg Med Chem Lett. 2017. PMID: 28254486
Balancing Properties with Carboxylates: A Lead Optimization Campaign for Selective and Orally Active CDK9 Inhibitors.
Tong Y, Florjancic AS, Clark RF, Lai C, Mastracchio A, Zhu GD, Smith ML, Kovar PJ, Shaw B, Albert DH, Qiu W, Longenecker KL, Liu X, Olson AM, Osterling DJ, Tahir SK, Phillips DC, Leverson JD, Souers AJ, Penning TD. Tong Y, et al. Among authors: clark rf. ACS Med Chem Lett. 2021 Jun 22;12(7):1108-1115. doi: 10.1021/acsmedchemlett.1c00161. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267880 Free PMC article.
SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT).
Curtin ML, Heyman HR, Clark RF, Sorensen BK, Doherty GA, Hansen TM, Frey RR, Sarris KA, Aguirre AL, Shrestha A, Tu N, Woller K, Pliushchev MA, Sweis RF, Cheng M, Wilsbacher JL, Kovar PJ, Guo J, Cheng D, Longenecker KL, Raich D, Korepanova AV, Soni NB, Algire MA, Richardson PL, Marin VL, Badagnani I, Vasudevan A, Buchanan FG, Maag D, Chiang GG, Tse C, Michaelides MR. Curtin ML, et al. Among authors: clark rf. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3317-3325. doi: 10.1016/j.bmcl.2017.06.018. Epub 2017 Jun 14. Bioorg Med Chem Lett. 2017. PMID: 28610984
Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors.
Wilsbacher JL, Cheng M, Cheng D, Trammell SAJ, Shi Y, Guo J, Koeniger SL, Kovar PJ, He Y, Selvaraju S, Heyman HR, Sorensen BK, Clark RF, Hansen TM, Longenecker KL, Raich D, Korepanova AV, Cepa S, Towne DL, Abraham VC, Tang H, Richardson PL, McLoughlin SM, Badagnani I, Curtin ML, Michaelides MR, Maag D, Buchanan FG, Chiang GG, Gao W, Rosenberg SH, Brenner C, Tse C. Wilsbacher JL, et al. Among authors: clark rf. Mol Cancer Ther. 2017 Jul;16(7):1236-1245. doi: 10.1158/1535-7163.MCT-16-0819. Epub 2017 May 3. Mol Cancer Ther. 2017. PMID: 28468779
Fragment-based discovery of a potent NAMPT inhibitor.
Korepanova A, Longenecker KL, Pratt SD, Panchal SC, Clark RF, Lake M, Gopalakrishnan SM, Raich D, Sun C, Petros AM. Korepanova A, et al. Among authors: clark rf. Bioorg Med Chem Lett. 2018 Feb 1;28(3):437-440. doi: 10.1016/j.bmcl.2017.12.023. Epub 2017 Dec 12. Bioorg Med Chem Lett. 2018. PMID: 29287958
A novel CDK9 inhibitor increases the efficacy of venetoclax (ABT-199) in multiple models of hematologic malignancies.
Phillips DC, Jin S, Gregory GP, Zhang Q, Xue J, Zhao X, Chen J, Tong Y, Zhang H, Smith M, Tahir SK, Clark RF, Penning TD, Devlin JR, Shortt J, Hsi ED, Albert DH, Konopleva M, Johnstone RW, Leverson JD, Souers AJ. Phillips DC, et al. Among authors: clark rf. Leukemia. 2020 Jun;34(6):1646-1657. doi: 10.1038/s41375-019-0652-0. Epub 2019 Dec 11. Leukemia. 2020. PMID: 31827241 Free PMC article.
Novel erythromycin derivatives with aryl groups tethered to the C-6 position are potent protein synthesis inhibitors and active against multidrug-resistant respiratory pathogens.
Ma Z, Clark RF, Brazzale A, Wang S, Rupp MJ, Li L, Griesgraber G, Zhang S, Yong H, Phan LT, Nemoto PA, Chu DT, Plattner JJ, Zhang X, Zhong P, Cao Z, Nilius AM, Shortridge VD, Flamm R, Mitten M, Meulbroek J, Ewing P, Alder J, Or YS. Ma Z, et al. Among authors: clark rf. J Med Chem. 2001 Nov 22;44(24):4137-56. doi: 10.1021/jm0102349. J Med Chem. 2001. PMID: 11708916
Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors.
Gu YG, Weitzberg M, Clark RF, Xu X, Li Q, Zhang T, Hansen TM, Liu G, Xin Z, Wang X, Wang R, McNally T, Zinker BA, Frevert EU, Camp HS, Beutel BA, Sham HL. Gu YG, et al. Among authors: clark rf. J Med Chem. 2006 Jun 29;49(13):3770-3. doi: 10.1021/jm060484v. J Med Chem. 2006. PMID: 16789734
311 results