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Page 1
Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9.
Phillipson LJ, Segal DH, Nero TL, Parker MW, Wan SS, de Silva M, Guthridge MA, Wei AH, Burns CJ. Phillipson LJ, et al. Among authors: segal dh. Bioorg Med Chem. 2015 Oct 1;23(19):6280-96. doi: 10.1016/j.bmc.2015.08.035. Epub 2015 Aug 28. Bioorg Med Chem. 2015. PMID: 26349627
Targeting acute myeloid leukemia by dual inhibition of PI3K signaling and Cdk9-mediated Mcl-1 transcription.
Thomas D, Powell JA, Vergez F, Segal DH, Nguyen NY, Baker A, Teh TC, Barry EF, Sarry JE, Lee EM, Nero TL, Jabbour AM, Pomilio G, Green BD, Manenti S, Glaser SP, Parker MW, Lopez AF, Ekert PG, Lock RB, Huang DC, Nilsson SK, Récher C, Wei AH, Guthridge MA. Thomas D, et al. Among authors: segal dh. Blood. 2013 Aug 1;122(5):738-48. doi: 10.1182/blood-2012-08-447441. Epub 2013 Jun 17. Blood. 2013. PMID: 23775716 Free article.
Enhancing venetoclax activity in acute myeloid leukemia by co-targeting MCL1.
Teh TC, Nguyen NY, Moujalled DM, Segal D, Pomilio G, Rijal S, Jabbour A, Cummins K, Lackovic K, Blombery P, Thompson E, Ekert PG, Lessene G, Glaser SP, Huang DCS, Roberts AW, Guthridge MA, Wei AH. Teh TC, et al. Leukemia. 2018 Feb;32(2):303-312. doi: 10.1038/leu.2017.243. Epub 2017 Jul 28. Leukemia. 2018. PMID: 28751770
Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors.
Sharp PP, Garnier JM, Hatfaludi T, Xu Z, Segal D, Jarman KE, Jousset H, Garnham A, Feutrill JT, Cuzzupe A, Hall P, Taylor S, Walkley CR, Tyler D, Dawson MA, Czabotar P, Wilks AF, Glaser S, Huang DCS, Burns CJ. Sharp PP, et al. ACS Med Chem Lett. 2017 Nov 14;8(12):1298-1303. doi: 10.1021/acsmedchemlett.7b00389. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259751 Free PMC article.
Simplified silvestrol analogues with potent cytotoxic activity.
Hawkins BC, Lindqvist LM, Nhu D, Sharp PP, Segal D, Powell AK, Campbell M, Ryan E, Chambers JM, White JM, Rizzacasa MA, Lessene G, Huang DC, Burns CJ. Hawkins BC, et al. ChemMedChem. 2014 Jul;9(7):1556-66. doi: 10.1002/cmdc.201400024. Epub 2014 Mar 27. ChemMedChem. 2014. PMID: 24677741
The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models.
Kotschy A, Szlavik Z, Murray J, Davidson J, Maragno AL, Le Toumelin-Braizat G, Chanrion M, Kelly GL, Gong JN, Moujalled DM, Bruno A, Csekei M, Paczal A, Szabo ZB, Sipos S, Radics G, Proszenyak A, Balint B, Ondi L, Blasko G, Robertson A, Surgenor A, Dokurno P, Chen I, Matassova N, Smith J, Pedder C, Graham C, Studeny A, Lysiak-Auvity G, Girard AM, Gravé F, Segal D, Riffkin CD, Pomilio G, Galbraith LC, Aubrey BJ, Brennan MS, Herold MJ, Chang C, Guasconi G, Cauquil N, Melchiore F, Guigal-Stephan N, Lockhart B, Colland F, Hickman JA, Roberts AW, Huang DC, Wei AH, Strasser A, Lessene G, Geneste O. Kotschy A, et al. Nature. 2016 Oct 27;538(7626):477-482. doi: 10.1038/nature19830. Epub 2016 Oct 19. Nature. 2016. PMID: 27760111
45 results