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Items: 29

1.

Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.

Smith A, Ni ZJ, Poon D, Huang Z, Chen Z, Zhang Q, Tandeske L, Merritt H, Shoemaker K, Chan J, Kaufman S, Huh K, Murray J, Appleton BA, Cowan-Jacob SW, Scheufler C, Kanazawa T, Jansen JM, Stuart D, Shafer CM.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5221-5224. doi: 10.1016/j.bmcl.2017.10.047. Epub 2017 Oct 20.

PMID:
29107542
2.

Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor.

Cho YS, Levell JR, Liu G, Caferro T, Sutton J, Shafer CM, Costales A, Manning JR, Zhao Q, Sendzik M, Shultz M, Chenail G, Dooley J, Villalba B, Farsidjani A, Chen J, Kulathila R, Xie X, Dodd S, Gould T, Liang G, Heimbach T, Slocum K, Firestone B, Pu M, Pagliarini R, Growney JD.

ACS Med Chem Lett. 2017 Sep 18;8(10):1116-1121. doi: 10.1021/acsmedchemlett.7b00342. eCollection 2017 Oct 12.

PMID:
29057061
3.

Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.

Wagman AS, Boyce RS, Brown SP, Fang E, Goff D, Jansen JM, Le VP, Levine BH, Ng SC, Ni ZJ, Nuss JM, Pfister KB, Ramurthy S, Renhowe PA, Ring DB, Shu W, Subramanian S, Zhou XA, Shafer CM, Harrison SD, Johnson KW, Bussiere DE.

J Med Chem. 2017 Oct 26;60(20):8482-8514. doi: 10.1021/acs.jmedchem.7b00922. Epub 2017 Oct 10.

PMID:
29016121
4.

Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design.

Han W, Ding Y, Xu Y, Pfister K, Zhu S, Warne B, Doyle M, Aikawa M, Amiri P, Appleton B, Stuart DD, Fanidi A, Shafer CM.

J Med Chem. 2016 Apr 14;59(7):3034-45. doi: 10.1021/acs.jmedchem.5b01657. Epub 2016 Mar 29.

PMID:
27002243
5.

Lineage Reprogramming of Fibroblasts into Proliferative Induced Cardiac Progenitor Cells by Defined Factors.

Lalit PA, Salick MR, Nelson DO, Squirrell JM, Shafer CM, Patel NG, Saeed I, Schmuck EG, Markandeya YS, Wong R, Lea MR, Eliceiri KW, Hacker TA, Crone WC, Kyba M, Garry DJ, Stewart R, Thomson JA, Downs KM, Lyons GE, Kamp TJ.

Cell Stem Cell. 2016 Mar 3;18(3):354-67. doi: 10.1016/j.stem.2015.12.001. Epub 2016 Feb 11.

6.

Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.

Williams TE, Subramanian S, Verhagen J, McBride CM, Costales A, Sung L, Antonios-McCrea W, McKenna M, Louie AK, Ramurthy S, Levine B, Shafer CM, Machajewski T, Renhowe PA, Appleton BA, Amiri P, Chou J, Stuart D, Aardalen K, Poon D.

ACS Med Chem Lett. 2015 Aug 3;6(9):961-5. doi: 10.1021/ml500526p. eCollection 2015 Sep 10.

7.

Discovery of Potent and Selective RSK Inhibitors as Biological Probes.

Jain R, Mathur M, Lan J, Costales A, Atallah G, Ramurthy S, Subramanian S, Setti L, Feucht P, Warne B, Doyle L, Basham S, Jefferson AB, Lindvall M, Appleton BA, Shafer CM.

J Med Chem. 2015 Sep 10;58(17):6766-83. doi: 10.1021/acs.jmedchem.5b00450. Epub 2015 Aug 13.

PMID:
26270416
8.

Correction to Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.

Subramanian S, Costales A, Williams TE, Levine B, McBride CM, Poon D, Amiri P, Renhowe PA, Shafer CM, Stuart D, Verhagen J, Ramurthy S.

ACS Med Chem Lett. 2014 Nov 25;5(12):1340. doi: 10.1021/ml500461g. eCollection 2014 Dec 11.

9.

Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990.

McBride CM, Levine B, Xia Y, Bellamacina C, Machajewski T, Gao Z, Renhowe P, Antonios-McCrea W, Barsanti P, Brinner K, Costales A, Doughan B, Lin X, Louie A, McKenna M, Mendenhall K, Poon D, Rico A, Wang M, Williams TE, Abrams T, Fong S, Hendrickson T, Lei D, Lin J, Menezes D, Pryer N, Taverna P, Xu Y, Zhou Y, Shafer CM.

J Med Chem. 2014 Nov 13;57(21):9124-9. doi: 10.1021/jm501107q. Epub 2014 Nov 4.

PMID:
25368984
10.

Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.

Subramanian S, Costales A, Williams TE, Levine B, McBride CM, Poon D, Amiri P, Renhowe PA, Shafer CM, Stuart D, Verhagen J, Ramurthy S.

ACS Med Chem Lett. 2014 Jul 17;5(9):989-92. doi: 10.1021/ml5002272. eCollection 2014 Sep 11. Erratum in: ACS Med Chem Lett. 2014 Dec 11;5(12):1340.

11.

Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers.

Aronchik I, Appleton BA, Basham SE, Crawford K, Del Rosario M, Doyle LV, Estacio WF, Lan J, Lindvall MK, Luu CA, Ornelas E, Venetsanakos E, Shafer CM, Jefferson AB.

Mol Cancer Res. 2014 May;12(5):803-12. doi: 10.1158/1541-7786.MCR-13-0595. Epub 2014 Feb 19.

12.

2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors.

Costales A, Mathur M, Ramurthy S, Lan J, Subramanian S, Jain R, Atallah G, Setti L, Lindvall M, Appleton BA, Ornelas E, Feucht P, Warne B, Doyle L, Basham SE, Aronchik I, Jefferson AB, Shafer CM.

Bioorg Med Chem Lett. 2014 Mar 15;24(6):1592-6. doi: 10.1016/j.bmcl.2014.01.058. Epub 2014 Jan 30.

PMID:
24534486
13.

Drug discovery considerations in the development of covalent inhibitors.

Mah R, Thomas JR, Shafer CM.

Bioorg Med Chem Lett. 2014 Jan 1;24(1):33-9. doi: 10.1016/j.bmcl.2013.10.003. Epub 2013 Oct 10. Review.

PMID:
24314671
14.

Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors.

Ramurthy S, Costales A, Jansen JM, Levine B, Renhowe PA, Shafer CM, Subramanian S.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1678-81. doi: 10.1016/j.bmcl.2011.12.112. Epub 2011 Dec 30.

PMID:
22264479
15.

3D Pharmacophore Model-Assisted Discovery of Novel CDC7 Inhibitors.

Lindvall M, McBride C, McKenna M, Gesner TG, Yabannavar A, Wong K, Lin S, Walter A, Shafer CM.

ACS Med Chem Lett. 2011 Aug 2;2(10):720-3. doi: 10.1021/ml200029w. eCollection 2011 Oct 13.

16.

Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors.

Ramurthy S, Aikawa M, Amiri P, Costales A, Hashash A, Jansen JM, Lin S, Ma S, Renhowe PA, Shafer CM, Subramanian S, Sung L, Verhagen J.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3286-9. doi: 10.1016/j.bmcl.2011.04.023. Epub 2011 Apr 14.

PMID:
21543226
17.

The quantitative potential for breast tomosynthesis imaging.

Shafer CM, Samei E, Lo JY.

Med Phys. 2010 Mar;37(3):1004-16.

18.

Synthesis and structure-activity relationships of bengazole A analogs.

Mulder RJ, Shafer CM, Dalisay DS, Molinski TF.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):2928-30. doi: 10.1016/j.bmcl.2009.04.069. Epub 2009 Apr 22. Erratum in: Bioorg Med Chem Lett. 2010 Sep 1;20(17):5361.

19.

Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.

Renhowe PA, Pecchi S, Shafer CM, Machajewski TD, Jazan EM, Taylor C, Antonios-McCrea W, McBride CM, Frazier K, Wiesmann M, Lapointe GR, Feucht PH, Warne RL, Heise CC, Menezes D, Aardalen K, Ye H, He M, Le V, Vora J, Jansen JM, Wernette-Hammond ME, Harris AL.

J Med Chem. 2009 Jan 22;52(2):278-92. doi: 10.1021/jm800790t.

PMID:
19113866
20.

Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.

Ramurthy S, Subramanian S, Aikawa M, Amiri P, Costales A, Dove J, Fong S, Jansen JM, Levine B, Ma S, McBride CM, Michaelian J, Pick T, Poon DJ, Girish S, Shafer CM, Stuart D, Sung L, Renhowe PA.

J Med Chem. 2008 Nov 27;51(22):7049-52. doi: 10.1021/jm801050k.

PMID:
18942827
21.

4-(1H-indazol-5-yl)-6-phenylpyrimidin-2(1H)-one analogs as potent CDC7 inhibitors.

Shafer CM, Lindvall M, Bellamacina C, Gesner TG, Yabannavar A, Jia W, Lin S, Walter A.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4482-5. doi: 10.1016/j.bmcl.2008.07.061. Epub 2008 Jul 17.

PMID:
18672368
22.

3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors.

McBride CM, Renhowe PA, Gesner TG, Jansen JM, Lin J, Ma S, Zhou Y, Shafer CM.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3789-92. Epub 2006 May 5.

PMID:
16678414
23.

Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases.

McBride CM, Renhowe PA, Heise C, Jansen JM, Lapointe G, Ma S, PiƱeda R, Vora J, Wiesmann M, Shafer CM.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9. Epub 2006 Apr 5.

PMID:
16603352
24.

Design and structure-activity relationship of heterocyclic analogs of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones as inhibitors of receptor tyrosine kinases.

Frazier K, Jazan E, McBride CM, Pecchi S, Renhowe PA, Shafer CM, Taylor C, Bussiere D, He MM, Jansen JM, Lapointe G, Ma S, Vora J, Wiesmann M.

Bioorg Med Chem Lett. 2006 Apr 15;16(8):2247-51. Epub 2006 Jan 30.

PMID:
16446087
25.

First Total Synthesis of Bengazole A.

Mulder RJ, Shafer CM, Molinski TF.

J Org Chem. 1999 Jun 25;64(13):4995-4998. No abstract available.

PMID:
11674590
26.

Monosubstituted Oxazoles. 1. Synthesis of 5-Substituted Oxazoles by Directed Alkylation.

Shafer CM, Molinski TF.

J Org Chem. 1998 Feb 6;63(3):551-555.

PMID:
11672044
27.

Mechanism for acivicin inactivation of triad glutamine amidotransferases.

Chittur SV, Klem TJ, Shafer CM, Davisson VJ.

Biochemistry. 2001 Jan 30;40(4):876-87.

PMID:
11170408
28.

First synthesis of bengazole A

Mulder RJ, Shafer CM, Molinski TF.

J Org Chem. 2000 Nov 17;65(23):8126. No abstract available.

PMID:
11073636
29.

Practical synthesis of 2,6-dideoxy-D-lyxo-hexose ("2-deoxy-D-fucose") from D-galactose.

Shafer CM, Molinski TF.

Carbohydr Res. 1998 Aug;310(4):223-8.

PMID:
9821260

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