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Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.
Man HW, Schafer P, Wong LM, Patterson RT, Corral LG, Raymon H, Blease K, Leisten J, Shirley MA, Tang Y, Babusis DM, Chen R, Stirling D, Muller GW. Man HW, et al. J Med Chem. 2009 Mar 26;52(6):1522-4. doi: 10.1021/jm900210d. J Med Chem. 2009. PMID: 19256507
Alpha-fluoro-substituted thalidomide analogues.
Man HW, Corral LG, Stirling DI, Muller GW. Man HW, et al. Bioorg Med Chem Lett. 2003 Oct 20;13(20):3415-7. doi: 10.1016/s0960-894x(03)00778-9. Bioorg Med Chem Lett. 2003. PMID: 14505639
Isosteric analogs of lenalidomide and pomalidomide: synthesis and biological activity.
Ruchelman AL, Man HW, Zhang W, Chen R, Capone L, Kang J, Parton A, Corral L, Schafer PH, Babusis D, Moghaddam MF, Tang Y, Shirley MA, Muller GW. Ruchelman AL, et al. Among authors: man hw. Bioorg Med Chem Lett. 2013 Jan 1;23(1):360-5. doi: 10.1016/j.bmcl.2012.10.071. Epub 2012 Oct 27. Bioorg Med Chem Lett. 2013. PMID: 23168019
Protein Degradation via CRL4CRBN Ubiquitin Ligase: Discovery and Structure-Activity Relationships of Novel Glutarimide Analogs That Promote Degradation of Aiolos and/or GSPT1.
Hansen JD, Condroski K, Correa M, Muller G, Man HW, Ruchelman A, Zhang W, Vocanson F, Crea T, Liu W, Lu G, Baculi F, LeBrun L, Mahmoudi A, Carmel G, Hickman M, Lu CC. Hansen JD, et al. Among authors: man hw. J Med Chem. 2018 Jan 25;61(2):492-503. doi: 10.1021/acs.jmedchem.6b01911. Epub 2017 Apr 13. J Med Chem. 2018. PMID: 28358507
A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos.
Matyskiela ME, Zhang W, Man HW, Muller G, Khambatta G, Baculi F, Hickman M, LeBrun L, Pagarigan B, Carmel G, Lu CC, Lu G, Riley M, Satoh Y, Schafer P, Daniel TO, Carmichael J, Cathers BE, Chamberlain PP. Matyskiela ME, et al. Among authors: man hw. J Med Chem. 2018 Jan 25;61(2):535-542. doi: 10.1021/acs.jmedchem.6b01921. Epub 2017 Apr 20. J Med Chem. 2018. PMID: 28425720
CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL.
Hagner PR, Man HW, Fontanillo C, Wang M, Couto S, Breider M, Bjorklund C, Havens CG, Lu G, Rychak E, Raymon H, Narla RK, Barnes L, Khambatta G, Chiu H, Kosek J, Kang J, Amantangelo MD, Waldman M, Lopez-Girona A, Cai T, Pourdehnad M, Trotter M, Daniel TO, Schafer PH, Klippel A, Thakurta A, Chopra R, Gandhi AK. Hagner PR, et al. Among authors: man hw. Blood. 2015 Aug 6;126(6):779-89. doi: 10.1182/blood-2015-02-628669. Epub 2015 May 22. Blood. 2015. PMID: 26002965 Free PMC article. Clinical Trial.
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