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Items: 12

1.

Structural Basis and Kinetic Pathway of RBM39 Recruitment to DCAF15 by a Sulfonamide Molecular Glue E7820.

Du X, Volkov OA, Czerwinski RM, Tan H, Huerta C, Morton ER, Rizzi JP, Wehn PM, Xu R, Nijhawan D, Wallace EM.

Structure. 2019 Nov 5;27(11):1625-1633.e3. doi: 10.1016/j.str.2019.10.005.

PMID:
31693911
2.

3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma.

Xu R, Wang K, Rizzi JP, Huang H, Grina JA, Schlachter ST, Wang B, Wehn PM, Yang H, Dixon DD, Czerwinski RM, Du X, Ged EL, Han G, Tan H, Wong T, Xie S, Josey JA, Wallace EM.

J Med Chem. 2019 Aug 8;62(15):6876-6893. doi: 10.1021/acs.jmedchem.9b00719. Epub 2019 Jul 8.

PMID:
31282155
3.

Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385).

Wehn PM, Rizzi JP, Dixon DD, Grina JA, Schlachter ST, Wang B, Xu R, Yang H, Du X, Han G, Wang K, Cao Z, Cheng T, Czerwinski RM, Goggin BS, Huang H, Halfmann MM, Maddie MA, Morton EL, Olive SR, Tan H, Xie S, Wong T, Josey JA, Wallace EM.

J Med Chem. 2018 Nov 8;61(21):9691-9721. doi: 10.1021/acs.jmedchem.8b01196. Epub 2018 Oct 18.

PMID:
30289716
4.

A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma.

Wallace EM, Rizzi JP, Han G, Wehn PM, Cao Z, Du X, Cheng T, Czerwinski RM, Dixon DD, Goggin BS, Grina JA, Halfmann MM, Maddie MA, Olive SR, Schlachter ST, Tan H, Wang B, Wang K, Xie S, Xu R, Yang H, Josey JA.

Cancer Res. 2016 Sep 15;76(18):5491-500. doi: 10.1158/0008-5472.CAN-16-0473. Epub 2016 Sep 6.

5.

Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.

Li Z, Wang X, Eksterowicz J, Gribble MW Jr, Alba GQ, Ayres M, Carlson TJ, Chen A, Chen X, Cho R, Connors RV, DeGraffenreid M, Deignan JT, Duquette J, Fan P, Fisher B, Fu J, Huard JN, Kaizerman J, Keegan KS, Li C, Li K, Li Y, Liang L, Liu W, Lively SE, Lo MC, Ma J, McMinn DL, Mihalic JT, Modi K, Ngo R, Pattabiraman K, Piper DE, Queva C, Ragains ML, Suchomel J, Thibault S, Walker N, Wang X, Wang Z, Wanska M, Wehn PM, Weidner MF, Zhang AJ, Zhao X, Kamb A, Wickramasinghe D, Dai K, McGee LR, Medina JC.

J Med Chem. 2014 Apr 24;57(8):3430-49. doi: 10.1021/jm500118j. Epub 2014 Apr 2.

PMID:
24641103
6.

Metabolism-guided discovery of a potent and orally bioavailable urea-based calcimimetic for the treatment of secondary hyperparathyroidism.

Wehn PM, Harrington PE, Carlson TJ, Davis J, Deprez P, Fotsch CH, Grillo MP, Lu JY, Morony S, Pattabiraman K, Poon SF, Reagan JD, St Jean DJ Jr, Temal T, Wang M, Yang Y, Henley C 3rd, Lively SE.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6625-8. doi: 10.1016/j.bmcl.2013.10.050. Epub 2013 Oct 31.

PMID:
24215889
7.

Facile synthesis of substituted 5-amino- and 3-amino-1,2,4-thiadiazoles from a common precursor.

Wehn PM, Harrington PE, Eksterowicz JE.

Org Lett. 2009 Dec 17;11(24):5666-9. doi: 10.1021/ol902371y.

PMID:
20000443
8.

A stereoselective synthesis of the bromopyrrole natural product (-)-agelastatin A.

Wehn PM, Du Bois J.

Angew Chem Int Ed Engl. 2009;48(21):3802-5. doi: 10.1002/anie.200806292.

9.

Exploring new uses for C-H amination: Ni-catalyzed cross-coupling of cyclic sulfamates.

Wehn PM, Du Bois J.

Org Lett. 2005 Oct 13;7(21):4685-8.

PMID:
16209510
10.

Stereochemical models for rh-catalyzed amination reactions of chiral sulfamates.

Wehn PM, Lee J, Du Bois J.

Org Lett. 2003 Dec 11;5(25):4823-6.

PMID:
14653683
11.

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