Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation

Search Page

Filters

My NCBI Filters

Text availability

Article attribute

Article type

Publication date

Search Results

12 results

Filters applied: . Clear all
Results are displayed in a computed author sort order. The Results By Year timeline is not available.
Page 1
Structure Overhaul Affords a Potent Purine PI3Kδ Inhibitor with Improved Tolerability.
Methot JL, Zhou H, Kattar SD, McGowan MA, Wilson K, Garcia Y, Deng Y, Altman M, Fradera X, Lesburg C, Fischmann T, Li C, Alves S, Shah S, Fernandez R, Goldenblatt P, Hill A, Shaffer L, Chen D, Tong V, McLeod RL, Yu H, Bass A, Kemper R, Gatto NT, LaFranco-Scheuch L, Trotter BW, Guzi T, Katz JD. Methot JL, et al. Among authors: goldenblatt p. J Med Chem. 2019 May 9;62(9):4370-4382. doi: 10.1021/acs.jmedchem.8b01818. Epub 2019 Apr 22. J Med Chem. 2019. PMID: 30986068
Design of selective PI3Kδ inhibitors using an iterative scaffold-hopping workflow.
Fradera X, Methot JL, Achab A, Christopher M, Altman MD, Zhou H, McGowan MA, Kattar SD, Wilson K, Garcia Y, Augustin MA, Lesburg CA, Shah S, Goldenblatt P, Katz JD. Fradera X, et al. Among authors: goldenblatt p. Bioorg Med Chem Lett. 2019 Sep 15;29(18):2575-2580. doi: 10.1016/j.bmcl.2019.08.004. Epub 2019 Aug 5. Bioorg Med Chem Lett. 2019. PMID: 31416665
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Zhou H, McGowan MA, Lipford K, Christopher M, Fradera X, Witter D, Lesburg CA, Li C, Methot JL, Lampe J, Achab A, Shaffer L, Goldenblatt P, Shah S, Bass A, Schroeder G, Chen D, Zeng H, Augustin MA, Katz JD. Zhou H, et al. Among authors: goldenblatt p. Bioorg Med Chem Lett. 2020 Jan 1;30(1):126715. doi: 10.1016/j.bmcl.2019.126715. Epub 2019 Oct 18. Bioorg Med Chem Lett. 2020. PMID: 31757666
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3Kδ Immunomodulators.
Methot JL, Zhou H, McGowan MA, Anthony NJ, Christopher M, Garcia Y, Achab A, Lipford K, Trotter BW, Altman MD, Fradera X, Lesburg CA, Li C, Alves S, Chappell CP, Jain R, Mangado R, Pinheiro E, Williams SMG, Goldenblatt P, Hill A, Shaffer L, Chen D, Tong V, McLeod RL, Lee HH, Yu H, Shah S, Katz JD. Methot JL, et al. Among authors: goldenblatt p. J Med Chem. 2021 Apr 22;64(8):5137-5156. doi: 10.1021/acs.jmedchem.1c00237. Epub 2021 Apr 2. J Med Chem. 2021. PMID: 33797901
Discovery of a new series of PI3K-δ inhibitors from Virtual Screening.
Fradera X, Deng Q, Achab A, Garcia Y, Kattar SD, McGowan MA, Methot JL, Wilson K, Zhou H, Shaffer L, Goldenblatt P, Tong V, Augustin MA, Altman MD, Lesburg CA, Shah S, Katz JD. Fradera X, et al. Among authors: goldenblatt p. Bioorg Med Chem Lett. 2021 Jun 15;42:128046. doi: 10.1016/j.bmcl.2021.128046. Epub 2021 Apr 16. Bioorg Med Chem Lett. 2021. PMID: 33865969
Optimization of Versatile Oxindoles as Selective PI3Kδ Inhibitors.
Methot JL, Achab A, Christopher M, Zhou H, McGowan MA, Trotter BW, Fradera X, Lesburg CA, Goldenblatt P, Hill A, Chen D, Otte KM, Augustin M, Shah S, Katz JD. Methot JL, et al. Among authors: goldenblatt p. ACS Med Chem Lett. 2020 Nov 19;11(12):2461-2469. doi: 10.1021/acsmedchemlett.0c00441. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335668 Free PMC article.
The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.
Siu T, Brubaker J, Fuller P, Torres L, Zeng H, Close J, Mampreian DM, Shi F, Liu D, Fradera X, Johnson K, Bays N, Kadic E, He F, Goldenblatt P, Shaffer L, Patel SB, Lesburg CA, Alpert C, Dorosh L, Deshmukh SV, Yu H, Klappenbach J, Elwood F, Dinsmore CJ, Fernandez R, Moy L, Young JR. Siu T, et al. Among authors: goldenblatt p. J Med Chem. 2017 Dec 14;60(23):9676-9690. doi: 10.1021/acs.jmedchem.7b01135. Epub 2017 Dec 4. J Med Chem. 2017. PMID: 29156136
Corrigendum to "Design of selective PI3Kδ inhibitors using an iterative scaffold-hopping workflow" [Bioorg. Med. Chem. Lett. 29 (2019) 2575-2580].
Fradera X, Methot JL, Achab A, Christopher M, Altman MD, Zhou H, McGowan MA, Kattar SD, Wilson K, Garcia Y, Augustin MA, Lesburg CA, Shah S, Goldenblatt P, Katz JD. Fradera X, et al. Among authors: goldenblatt p. Bioorg Med Chem Lett. 2020 Aug 15;30(16):127363. doi: 10.1016/j.bmcl.2020.127363. Epub 2020 Jun 23. Bioorg Med Chem Lett. 2020. PMID: 32591133 No abstract available.
Discovery of MK-4688: an Efficient Inhibitor of the HDM2-p53 Protein-Protein Interaction.
Reutershan MH, Machacek MR, Altman MD, Bogen S, Cai M, Cammarano C, Chen D, Christopher M, Cryan J, Daublain P, Fradera X, Geda P, Goldenblatt P, Hill AD, Kemper RA, Kutilek V, Li C, Martinez M, McCoy M, Nair L, Pan W, Thompson CF, Scapin G, Shizuka M, Spatz ML, Steinhuebel D, Sun B, Voss ME, Wang X, Yang L, Yeh TC, Dussault I, Marshall CG, Trotter BW. Reutershan MH, et al. Among authors: goldenblatt p. J Med Chem. 2021 Nov 11;64(21):16213-16241. doi: 10.1021/acs.jmedchem.1c01524. Epub 2021 Oct 29. J Med Chem. 2021. PMID: 34714078
Discovery and characterization of novel peptide inhibitors of the NRF2/MAFG/DNA ternary complex for the treatment of cancer.
Simov V, Altman MD, Bianchi E, DelRizzo S, DiNunzio EN, Feng G, Goldenblatt P, Ingenito R, Johnson SA, Mansueto MS, Mayhood T, Mortison JD, Serebrov V, Sondey C, Sriraman V, Tucker TJ, Walji A, Wan H, Yue Y, Stoeck A, DiMauro EF. Simov V, et al. Among authors: goldenblatt p. Eur J Med Chem. 2021 Nov 15;224:113686. doi: 10.1016/j.ejmech.2021.113686. Epub 2021 Jul 7. Eur J Med Chem. 2021. PMID: 34303079
12 results