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Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide.
Zehnder L, Bennett M, Meng J, Huang B, Ninkovic S, Wang F, Braganza J, Tatlock J, Jewell T, Zhou JZ, Burke B, Wang J, Maegley K, Mehta PP, Yin MJ, Gajiwala KS, Hickey MJ, Yamazaki S, Smith E, Kang P, Sistla A, Dovalsantos E, Gehring MR, Kania R, Wythes M, Kung PP. Zehnder L, et al. Among authors: maegley k. J Med Chem. 2011 May 12;54(9):3368-85. doi: 10.1021/jm200128m. Epub 2011 Apr 20. J Med Chem. 2011. PMID: 21438541
Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.
Canan Koch SS, Thoresen LH, Tikhe JG, Maegley KA, Almassy RJ, Li J, Yu XH, Zook SE, Kumpf RA, Zhang C, Boritzki TJ, Mansour RN, Zhang KE, Ekker A, Calabrese CR, Curtin NJ, Kyle S, Thomas HD, Wang LZ, Calvert AH, Golding BT, Griffin RJ, Newell DR, Webber SE, Hostomsky Z. Canan Koch SS, et al. J Med Chem. 2002 Nov 7;45(23):4961-74. doi: 10.1021/jm020259n. J Med Chem. 2002. PMID: 12408707
Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.
Skalitzky DJ, Marakovits JT, Maegley KA, Ekker A, Yu XH, Hostomsky Z, Webber SE, Eastman BW, Almassy R, Li J, Curtin NJ, Newell DR, Calvert AH, Griffin RJ, Golding BT. Skalitzky DJ, et al. J Med Chem. 2003 Jan 16;46(2):210-3. doi: 10.1021/jm0255769. J Med Chem. 2003. PMID: 12519059
Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.
Tikhe JG, Webber SE, Hostomsky Z, Maegley KA, Ekkers A, Li J, Yu XH, Almassy RJ, Kumpf RA, Boritzki TJ, Zhang C, Calabrese CR, Curtin NJ, Kyle S, Thomas HD, Wang LZ, Calvert AH, Golding BT, Griffin RJ, Newell DR. Tikhe JG, et al. J Med Chem. 2004 Oct 21;47(22):5467-81. doi: 10.1021/jm030513r. J Med Chem. 2004. PMID: 15481984
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.
Kung PP, Funk L, Meng J, Collins M, Zhou JZ, Johnson MC, Ekker A, Wang J, Mehta P, Yin MJ, Rodgers C, Davies JF 2nd, Bayman E, Smeal T, Maegley KA, Gehring MR. Kung PP, et al. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6273-8. doi: 10.1016/j.bmcl.2008.09.081. Epub 2008 Sep 26. Bioorg Med Chem Lett. 2008. PMID: 18929486
Ack1: activation and regulation by allostery.
Gajiwala KS, Maegley K, Ferre R, He YA, Yu X. Gajiwala KS, et al. Among authors: maegley k. PLoS One. 2013;8(1):e53994. doi: 10.1371/journal.pone.0053994. Epub 2013 Jan 14. PLoS One. 2013. PMID: 23342057 Free PMC article.
39 results