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 Custom Filters

Publication date

Text availability

Article attribute

Article type

Additional filters

Article Language

Species

Sex

Age

Other

Search Results

130 results

Filters applied: . Clear all
Results are displayed in a computed author sort order. The Publication Date timeline is not available.
Page 1
Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers.
Freeman DB, Hopkins TD, Mikochik PJ, Vacca JP, Gao H, Naylor-Olsen A, Rudra S, Li H, Pop MS, Villagomez RA, Lee C, Li H, Zhou M, Saffran DC, Rioux N, Hood TR, Day MAL, McKeown MR, Lin CY, Bischofberger N, Trotter BW. Freeman DB, et al. Among authors: vacca jp. J Med Chem. 2023 Dec 14;66(23):15629-15647. doi: 10.1021/acs.jmedchem.3c01233. Epub 2023 Nov 15. J Med Chem. 2023. PMID: 37967851 Free PMC article.
Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors.
Richters A, Doyle SK, Freeman DB, Lee C, Leifer BS, Jagannathan S, Kabinger F, Koren JV, Struntz NB, Urgiles J, Stagg RA, Curtin BH, Chatterjee D, Mathea S, Mikochik PJ, Hopkins TD, Gao H, Branch JR, Xin H, Westover L, Bignan GC, Rupnow BA, Karlin KL, Olson CM, Westbrook TF, Vacca J, Wilfong CM, Trotter BW, Saffran DC, Bischofberger N, Knapp S, Russo JW, Hickson I, Bischoff JR, Gottardis MM, Balk SP, Lin CY, Pop MS, Koehler AN. Richters A, et al. Cell Chem Biol. 2021 Feb 18;28(2):134-147.e14. doi: 10.1016/j.chembiol.2020.10.001. Epub 2020 Oct 20. Cell Chem Biol. 2021. PMID: 33086052 Free article.
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.
Tucker TJ, Lumma WC, Lewis SD, Gardell SJ, Lucas BJ, Sisko JT, Lynch JJ, Lyle EA, Baskin EP, Woltmann RF, Appleby SD, Chen IW, Dancheck KB, Naylor-Olsen AM, Krueger JA, Cooper CM, Vacca JP. Tucker TJ, et al. Among authors: vacca jp. J Med Chem. 1997 Oct 24;40(22):3687-93. doi: 10.1021/jm970397q. J Med Chem. 1997. PMID: 9357536
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.
Sanderson PE, Cutrona KJ, Dorsey BD, Dyer DL, McDonough CM, Naylor-Olsen AM, Chen IW, Chen Z, Cook JJ, Gardell SJ, Krueger JA, Lewis SD, Lin JH, Lucas BJ Jr, Lyle EA, Lynch JJ Jr, Stranieri MT, Vastag K, Shafer JA, Vacca JP. Sanderson PE, et al. Among authors: vacca jp. Bioorg Med Chem Lett. 1998 Apr 7;8(7):817-22. doi: 10.1016/s0960-894x(98)00117-6. Bioorg Med Chem Lett. 1998. PMID: 9871547
Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.
Brady SF, Stauffer KJ, Lumma WC, Smith GM, Ramjit HG, Lewis SD, Lucas BJ, Gardell SJ, Lyle EA, Appleby SD, Cook JJ, Holahan MA, Stranieri MT, Lynch JJ Jr, Lin JH, Chen IW, Vastag K, Naylor-Olsen AM, Vacca JP. Brady SF, et al. Among authors: vacca jp. J Med Chem. 1998 Jan 29;41(3):401-6. doi: 10.1021/jm9705014. J Med Chem. 1998. PMID: 9464370
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.
Feng DM, Gardell SJ, Lewis SD, Bock MG, Chen Z, Freidinger RM, Naylor-Olsen AM, Ramjit HG, Woltmann R, Baskin EP, Lynch JJ, Lucas R, Shafer JA, Dancheck KB, Chen IW, Mao SS, Krueger JA, Hare TR, Mulichak AM, Vacca JP. Feng DM, et al. Among authors: vacca jp. J Med Chem. 1997 Nov 7;40(23):3726-33. doi: 10.1021/jm970493r. J Med Chem. 1997. PMID: 9371237
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.
Tucker TJ, Brady SF, Lumma WC, Lewis SD, Gardell SJ, Naylor-Olsen AM, Yan Y, Sisko JT, Stauffer KJ, Lucas BJ, Lynch JJ, Cook JJ, Stranieri MT, Holahan MA, Lyle EA, Baskin EP, Chen IW, Dancheck KB, Krueger JA, Cooper CM, Vacca JP. Tucker TJ, et al. Among authors: vacca jp. J Med Chem. 1998 Aug 13;41(17):3210-9. doi: 10.1021/jm9801713. J Med Chem. 1998. PMID: 9703466
C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.
Isaacs RC, Cutrona KJ, Newton CL, Sanderson PE, Solinsky MG, Baskin EP, Chen IW, Cooper CM, Cook JJ, Gardell SJ, Lewis SD, Lucas RJ Jr, Lyle EA, Lynch JJ Jr, Naylor-Olsen AM, Stranieri MT, Vastag K, Vacca JP. Isaacs RC, et al. Among authors: vacca jp. Bioorg Med Chem Lett. 1998 Jul 7;8(13):1719-24. doi: 10.1016/s0960-894x(98)00297-2. Bioorg Med Chem Lett. 1998. PMID: 9873422
130 results