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Discovery and SAR of Novel Disubstituted Quinazolines as Dual PI3Kalpha/mTOR Inhibitors Targeting Breast Cancer.
ACS Med Chem Lett. 2020 Oct 12;11(11):2156-2164. doi: 10.1021/acsmedchemlett.0c00289. eCollection 2020 Nov 12.
ACS Med Chem Lett. 2020.
PMID: 33214824
Free PMC article.
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.
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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
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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
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N-methyl-D-aspartate antagonists and neuropathic pain: the search for relief.
Childers WE Jr, Baudy RB.
Childers WE Jr, et al.
J Med Chem. 2007 May 31;50(11):2557-62. doi: 10.1021/jm060728b. Epub 2007 May 10.
J Med Chem. 2007.
PMID: 17489572
Review.
No abstract available.
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Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan.
Childers WE Jr, Abou-Gharbia MA, Kelly MG, Andree TH, Harrison BL, Ho DM, Hornby G, Huryn DM, Potestio L, Rosenzweig-Lipson SJ, Schmid J, Smith DL, Sukoff SJ, Zhang G, Schechter LE.
Childers WE Jr, et al.
J Med Chem. 2005 May 19;48(10):3467-70. doi: 10.1021/jm049493z.
J Med Chem. 2005.
PMID: 15887953
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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
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