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Page 1
Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.
Pecchi S, Ni ZJ, Han W, Smith A, Lan J, Burger M, Merritt H, Wiesmann M, Chan J, Kaufman S, Knapp MS, Janssen J, Huh K, Voliva CF. Pecchi S, et al. Among authors: voliva cf. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4652-6. doi: 10.1016/j.bmcl.2013.06.010. Epub 2013 Jun 12. Bioorg Med Chem Lett. 2013. PMID: 23820386
Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.
Pecchi S, Renhowe PA, Taylor C, Kaufman S, Merritt H, Wiesmann M, Shoemaker KR, Knapp MS, Ornelas E, Hendrickson TF, Fantl W, Voliva CF. Pecchi S, et al. Among authors: voliva cf. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6895-8. doi: 10.1016/j.bmcl.2010.10.021. Epub 2010 Oct 13. Bioorg Med Chem Lett. 2010. PMID: 21035331
Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors.
Burger MT, Knapp M, Wagman A, Ni ZJ, Hendrickson T, Atallah G, Zhang Y, Frazier K, Verhagen J, Pfister K, Ng S, Smith A, Bartulis S, Merrit H, Weismann M, Xin X, Haznedar J, Voliva CF, Iwanowicz E, Pecchi S. Burger MT, et al. Among authors: voliva cf. ACS Med Chem Lett. 2010 Oct 13;2(1):34-8. doi: 10.1021/ml1001932. eCollection 2011 Jan 13. ACS Med Chem Lett. 2010. PMID: 24900252 Free PMC article.
Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.
Burger MT, Pecchi S, Wagman A, Ni ZJ, Knapp M, Hendrickson T, Atallah G, Pfister K, Zhang Y, Bartulis S, Frazier K, Ng S, Smith A, Verhagen J, Haznedar J, Huh K, Iwanowicz E, Xin X, Menezes D, Merritt H, Lee I, Wiesmann M, Kaufman S, Crawford K, Chin M, Bussiere D, Shoemaker K, Zaror I, Maira SM, Voliva CF. Burger MT, et al. Among authors: voliva cf. ACS Med Chem Lett. 2011 Aug 26;2(10):774-9. doi: 10.1021/ml200156t. eCollection 2011 Oct 13. ACS Med Chem Lett. 2011. PMID: 24900266 Free PMC article.
Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.
Han W, Menezes DL, Xu Y, Knapp MS, Elling R, Burger MT, Ni ZJ, Smith A, Lan J, Williams TE, Verhagen J, Huh K, Merritt H, Chan J, Kaufman S, Voliva CF, Pecchi S. Han W, et al. Among authors: voliva cf. Bioorg Med Chem Lett. 2016 Feb 1;26(3):742-746. doi: 10.1016/j.bmcl.2016.01.003. Epub 2016 Jan 5. Bioorg Med Chem Lett. 2016. PMID: 26774655
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.
Karpov AS, Amiri P, Bellamacina C, Bellance MH, Breitenstein W, Daniel D, Denay R, Fabbro D, Fernandez C, Galuba I, Guerro-Lagasse S, Gutmann S, Hinh L, Jahnke W, Klopp J, Lai A, Lindvall MK, Ma S, Möbitz H, Pecchi S, Rummel G, Shoemaker K, Trappe J, Voliva C, Cowan-Jacob SW, Marzinzik AL. Karpov AS, et al. ACS Med Chem Lett. 2015 May 22;6(7):776-81. doi: 10.1021/acsmedchemlett.5b00102. eCollection 2015 Jul 9. ACS Med Chem Lett. 2015. PMID: 26191365 Free PMC article.
Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor.
Maira SM, Pecchi S, Huang A, Burger M, Knapp M, Sterker D, Schnell C, Guthy D, Nagel T, Wiesmann M, Brachmann S, Fritsch C, Dorsch M, Chène P, Shoemaker K, De Pover A, Menezes D, Martiny-Baron G, Fabbro D, Wilson CJ, Schlegel R, Hofmann F, García-Echeverría C, Sellers WR, Voliva CF. Maira SM, et al. Among authors: voliva cf. Mol Cancer Ther. 2012 Feb;11(2):317-28. doi: 10.1158/1535-7163.MCT-11-0474. Epub 2011 Dec 21. Mol Cancer Ther. 2012. PMID: 22188813
23 results