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Estrogen receptor antagonists are anti-cryptococcal agents that directly bind EF hand proteins and synergize with fluconazole in vivo.
Butts A, Koselny K, Chabrier-Roselló Y, Semighini CP, Brown JC, Wang X, Annadurai S, DiDone L, Tabroff J, Childers WE Jr, Abou-Gharbia M, Wellington M, Cardenas ME, Madhani HD, Heitman J, Krysan DJ. Butts A, et al. Among authors: childers we jr. mBio. 2014 Feb 11;5(1):e00765-13. doi: 10.1128/mBio.00765-13. mBio. 2014. PMID: 24520056 Free PMC article.
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
Childers WE Jr, Havran LM, Asselin M, Bicksler JJ, Chong DC, Grosu GT, Shen Z, Abou-Gharbia MA, Bach AC 3rd, Harrison BL, Kagan N, Kleintop T, Magolda R, Marathias V, Robichaud AJ, Sabb AL, Zhang MY, Andree TH, Aschmies SH, Beyer C, Comery TA, Day M, Grauer SM, Hughes ZA, Rosenzweig-Lipson S, Platt B, Pulicicchio C, Smith DE, Sukoff-Rizzo SJ, Sullivan KM, Adedoyin A, Huselton C, Hirst WD. Childers WE Jr, et al. J Med Chem. 2010 May 27;53(10):4066-84. doi: 10.1021/jm1000908. J Med Chem. 2010. PMID: 20443629
Prodrugs of perzinfotel with improved oral bioavailability.
Baudy RB, Butera JA, Abou-Gharbia MA, Chen H, Harrison B, Jain U, Magolda R, Sze JY, Brandt MR, Cummons TA, Kowal D, Pangalos MN, Zupan B, Hoffmann M, May M, Mugford C, Kennedy J, Childers WE Jr. Baudy RB, et al. Among authors: childers we jr. J Med Chem. 2009 Feb 12;52(3):771-8. doi: 10.1021/jm8011799. J Med Chem. 2009. PMID: 19146418
Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents.
Abou-Gharbia MA, Childers WE Jr, Fletcher H, McGaughey G, Patel U, Webb MB, Yardley J, Andree T, Boast C, Kucharik RJ Jr, Marquis K, Morris H, Scerni R, Moyer JA. Abou-Gharbia MA, et al. Among authors: childers we jr. J Med Chem. 1999 Dec 16;42(25):5077-94. doi: 10.1021/jm9806704. J Med Chem. 1999. PMID: 10602693