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Page 1
Conformational refinement of hydroxamate-based histone deacetylase inhibitors and exploration of 3-piperidin-3-ylindole analogues of dacinostat (LAQ824).
Cho YS, Whitehead L, Li J, Chen CH, Jiang L, Vögtle M, Francotte E, Richert P, Wagner T, Traebert M, Lu Q, Cao X, Dumotier B, Fejzo J, Rajan S, Wang P, Yan-Neale Y, Shao W, Atadja P, Shultz M. Cho YS, et al. Among authors: whitehead l. J Med Chem. 2010 Apr 8;53(7):2952-63. doi: 10.1021/jm100007m. J Med Chem. 2010. PMID: 20205394
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
Shultz MD, Cao X, Chen CH, Cho YS, Davis NR, Eckman J, Fan J, Fekete A, Firestone B, Flynn J, Green J, Growney JD, Holmqvist M, Hsu M, Jansson D, Jiang L, Kwon P, Liu G, Lombardo F, Lu Q, Majumdar D, Meta C, Perez L, Pu M, Ramsey T, Remiszewski S, Skolnik S, Traebert M, Urban L, Uttamsingh V, Wang P, Whitebread S, Whitehead L, Yan-Neale Y, Yao YM, Zhou L, Atadja P. Shultz MD, et al. Among authors: whitehead l. J Med Chem. 2011 Jul 14;54(13):4752-72. doi: 10.1021/jm200388e. Epub 2011 Jun 17. J Med Chem. 2011. PMID: 21650221
Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.
Whitehead L, Dobler MR, Radetich B, Zhu Y, Atadja PW, Claiborne T, Grob JE, McRiner A, Pancost MR, Patnaik A, Shao W, Shultz M, Tichkule R, Tommasi RA, Vash B, Wang P, Stams T. Whitehead L, et al. Bioorg Med Chem. 2011 Aug 1;19(15):4626-34. doi: 10.1016/j.bmc.2011.06.030. Epub 2011 Jun 15. Bioorg Med Chem. 2011. PMID: 21723733
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
Shultz M, Fan J, Chen C, Cho YS, Davis N, Bickford S, Buteau K, Cao X, Holmqvist M, Hsu M, Jiang L, Liu G, Lu Q, Patel C, Suresh JR, Selvaraj M, Urban L, Wang P, Yan-Neale Y, Whitehead L, Zhang H, Zhou L, Atadja P. Shultz M, et al. Among authors: whitehead l. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4909-12. doi: 10.1016/j.bmcl.2011.06.015. Bioorg Med Chem Lett. 2011. PMID: 21742496
Antibacterial optimization of 4-aminothiazolyl analogues of the natural product GE2270 A: identification of the cycloalkylcarboxylic acids.
LaMarche MJ, Leeds JA, Amaral K, Brewer JT, Bushell SM, Dewhurst JM, Dzink-Fox J, Gangl E, Goldovitz J, Jain A, Mullin S, Neckermann G, Osborne C, Palestrant D, Patane MA, Rann EM, Sachdeva M, Shao J, Tiamfook S, Whitehead L, Yu D. LaMarche MJ, et al. Among authors: whitehead l. J Med Chem. 2011 Dec 8;54(23):8099-109. doi: 10.1021/jm200938f. Epub 2011 Nov 1. J Med Chem. 2011. PMID: 21999529
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
LaMarche MJ, Leeds JA, Amaral A, Brewer JT, Bushell SM, Deng G, Dewhurst JM, Ding J, Dzink-Fox J, Gamber G, Jain A, Lee K, Lee L, Lister T, McKenney D, Mullin S, Osborne C, Palestrant D, Patane MA, Rann EM, Sachdeva M, Shao J, Tiamfook S, Trzasko A, Whitehead L, Yifru A, Yu D, Yan W, Zhu Q. LaMarche MJ, et al. Among authors: whitehead l. J Med Chem. 2012 Mar 8;55(5):2376-87. doi: 10.1021/jm201685h. Epub 2012 Feb 23. J Med Chem. 2012. PMID: 22315981
Antibacterial and Solubility Optimization of Thiomuracin A.
LaMarche MJ, Leeds JA, Brewer J, Dean K, Ding J, Dzink-Fox J, Gamber G, Jain A, Kerrigan R, Krastel P, Lee K, Lombardo F, McKenney D, Neckermann G, Osborne C, Palestrant D, Patane MA, Rann EM, Robinson Z, Schmitt E, Stams T, Tiamfook S, Yu D, Whitehead L. LaMarche MJ, et al. Among authors: whitehead l. J Med Chem. 2016 Jul 28;59(14):6920-8. doi: 10.1021/acs.jmedchem.6b00726. Epub 2016 Jul 12. J Med Chem. 2016. PMID: 27355833
Avoidance of the Ames test liability for aryl-amines via computation.
McCarren P, Bebernitz GR, Gedeck P, Glowienke S, Grondine MS, Kirman LC, Klickstein J, Schuster HF, Whitehead L. McCarren P, et al. Among authors: whitehead l. Bioorg Med Chem. 2011 May 15;19(10):3173-82. doi: 10.1016/j.bmc.2011.03.066. Epub 2011 Apr 3. Bioorg Med Chem. 2011. PMID: 21524589
456 results