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Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines.
Kaizerman JA, Aaron W, An S, Austin R, Brown M, Chong A, Huang T, Hungate R, Jiang B, Johnson MG, Lee G, Lucas BS, Orf J, Rong M, Toteva MM, Wickramasinghe D, Xu G, Ye Q, Zhong W, McMinn DL. Kaizerman JA, et al. Among authors: aaron w. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4607-10. doi: 10.1016/j.bmcl.2010.06.006. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20594845
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.
Brown ML, Aaron W, Austin RJ, Chong A, Huang T, Jiang B, Kaizerman JA, Lee G, Lucas BS, McMinn DL, Orf J, Rong M, Toteva MM, Xu G, Ye Q, Zhong W, Degraffenreid MR, Wickramasinghe D, Powers JP, Hungate R, Johnson MG. Brown ML, et al. Among authors: aaron w. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5206-9. doi: 10.1016/j.bmcl.2011.07.052. Epub 2011 Jul 23. Bioorg Med Chem Lett. 2011. PMID: 21840217
Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists.
Lucas BS, Aaron W, An S, Austin RJ, Brown M, Chan H, Chong A, Hungate R, Huang T, Jiang B, Johnson MG, Kaizerman JA, Lee G, McMinn DL, Orf J, Powers JP, Rong M, Toteva MM, Uyeda C, Wickramasinghe D, Xu G, Ye Q, Zhong W. Lucas BS, et al. Among authors: aaron w. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3618-22. doi: 10.1016/j.bmcl.2010.04.110. Epub 2010 Apr 28. Bioorg Med Chem Lett. 2010. PMID: 20493695
Preclinical Characterization of HPN536, a Trispecific, T-Cell-Activating Protein Construct for the Treatment of Mesothelin-Expressing Solid Tumors.
Molloy ME, Austin RJ, Lemon BD, Aaron WH, Ganti V, Jones A, Jones SD, Strobel KL, Patnaik P, Sexton K, Tatalick L, Yu TZ, Baeuerle PA, Law CL, Wesche H. Molloy ME, et al. Among authors: aaron wh. Clin Cancer Res. 2021 Mar 1;27(5):1452-1462. doi: 10.1158/1078-0432.CCR-20-3392. Epub 2020 Dec 1. Clin Cancer Res. 2021. PMID: 33262134
21 results