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Items: 20

1.

Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors.

Bisi JE, Sorrentino JA, Jordan JL, Darr DD, Roberts PJ, Tavares FX, Strum JC.

Oncotarget. 2017 Jun 27;8(26):42343-42358. doi: 10.18632/oncotarget.16216.

2.

Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression.

Bisi JE, Sorrentino JA, Roberts PJ, Tavares FX, Strum JC.

Mol Cancer Ther. 2016 May;15(5):783-93. doi: 10.1158/1535-7163.MCT-15-0775. Epub 2016 Jan 29.

3.

Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy.

Thomson SA, Banker P, Bickett DM, Boucheron JA, Carter HL, Clancy DC, Cooper JP, Dickerson SH, Garrido DM, Nolte RT, Peat AJ, Sheckler LR, Sparks SM, Tavares FX, Wang L, Wang TY, Weiel JE.

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1177-82. doi: 10.1016/j.bmcl.2008.12.085. Epub 2008 Dec 25.

PMID:
19138846
4.

Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of Type 2 diabetes: 2. Optimization of serine and threonine ether amino acid residues.

Sparks SM, Banker P, Bickett DM, Clancy DC, Dickerson SH, Garrido DM, Golden PL, Peat AJ, Sheckler LR, Tavares FX, Thomson SA, Weiel JE.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):981-5. doi: 10.1016/j.bmcl.2008.11.084. Epub 2008 Nov 27.

PMID:
19095443
5.

Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes: 1. Identification of 1-amino-1-cycloalkyl carboxylic acid headgroups.

Sparks SM, Banker P, Bickett DM, Carter HL, Clancy DC, Dickerson SH, Dwornik KA, Garrido DM, Golden PL, Nolte RT, Peat AJ, Sheckler LR, Tavares FX, Thomson SA, Wang L, Weiel JE.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):976-80. doi: 10.1016/j.bmcl.2008.11.085. Epub 2008 Nov 27.

PMID:
19095442
6.

Acyclic, orally bioavailable ketone-based cathepsin K inhibitors.

Barrett DG, Catalano JG, Deaton DN, Long ST, McFadyen RB, Miller AB, Miller LR, Samano V, Tavares FX, Wells-Knecht KJ, Wright LL, Zhou HQ.

Bioorg Med Chem Lett. 2007 Jan 1;17(1):22-7. Epub 2006 Nov 17.

PMID:
17157021
7.

6-(4-chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-based melanin-concentrating hormone receptor 1 antagonist.

Tavares FX, Al-Barazanji KA, Bishop MJ, Britt CS, Carlton DL, Cooper JP, Feldman PL, Garrido DM, Goetz AS, Grizzle MK, Hertzog DL, Ignar DM, Lang DG, McIntyre MS, Ott RJ, Peat AJ, Zhou HQ.

J Med Chem. 2006 Nov 30;49(24):7108-18.

PMID:
17125263
8.

Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1.

Tavares FX, Al-Barazanji KA, Bigham EC, Bishop MJ, Britt CS, Carlton DL, Feldman PL, Goetz AS, Grizzle MK, Guo YC, Handlon AL, Hertzog DL, Ignar DM, Lang DG, Ott RJ, Peat AJ, Zhou HQ.

J Med Chem. 2006 Nov 30;49(24):7095-107.

PMID:
17125262
9.

The discovery and optimization of pyrimidinone-containing MCH R1 antagonists.

Hertzog DL, Al-Barazanji KA, Bigham EC, Bishop MJ, Britt CS, Carlton DL, Cooper JP, Daniels AJ, Garrido DM, Goetz AS, Grizzle MK, Guo YC, Handlon AL, Ignar DM, Morgan RO, Peat AJ, Tavares FX, Zhou H.

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4723-7. Epub 2006 Jul 25.

PMID:
16870432
10.

Design of cathepsin K inhibitors for osteoporosis.

Deaton DN, Tavares FX.

Curr Top Med Chem. 2005;5(16):1639-75. Review.

PMID:
16375747
11.

Editorial.

Tavares FX.

Curr Top Med Chem. 2005;5(16):1587. No abstract available.

PMID:
16375743
12.

Ketoheterocycle-based inhibitors of cathepsin K: a novel entry into the synthesis of peptidic ketoheterocycles.

Tavares FX, Deaton DN, Miller AB, Miller LR, Wright LL.

Bioorg Med Chem Lett. 2005 Sep 1;15(17):3891-5.

PMID:
15993587
13.

P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.

Barrett DG, Boncek VM, Catalano JG, Deaton DN, Hassell AM, Jurgensen CH, Long ST, McFadyen RB, Miller AB, Miller LR, Payne JA, Ray JA, Samano V, Shewchuk LM, Tavares FX, Wells-Knecht KJ, Willard DH Jr, Wright LL, Zhou HQ.

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3540-6.

PMID:
15982880
14.

Novel and potent cyclic cyanamide-based cathepsin K inhibitors.

Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Shewchuk LM, Tavares FX, Willard DH Jr, Wright LL.

Bioorg Med Chem Lett. 2005 Apr 1;15(7):1815-9.

PMID:
15780613
15.

Ketoamide-based inhibitors of cysteine protease, cathepsin K: P3 modifications.

Tavares FX, Deaton DN, Miller LR, Wright LL.

J Med Chem. 2004 Oct 7;47(21):5057-68.

PMID:
15456249
16.

Potent and selective ketoamide-based inhibitors of cysteine protease, cathepsin K.

Tavares FX, Deaton DN, Miller AB, Miller LR, Wright LL, Zhou HQ.

J Med Chem. 2004 Oct 7;47(21):5049-56.

PMID:
15456248
17.

N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy.

Tavares FX, Boucheron JA, Dickerson SH, Griffin RJ, Preugschat F, Thomson SA, Wang TY, Zhou HQ.

J Med Chem. 2004 Sep 9;47(19):4716-30.

PMID:
15341487
18.

Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K.

Barrett DG, Catalano JG, Deaton DN, Long ST, Miller LR, Tavares FX, Wells-Knecht KJ, Wright LL, Zhou HQ.

Bioorg Med Chem Lett. 2004 May 17;14(10):2543-6.

PMID:
15109647
19.

Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin k.

Tavares FX, Boncek V, Deaton DN, Hassell AM, Long ST, Miller AB, Payne AA, Miller LR, Shewchuk LM, Wells-Knecht K, Willard DH Jr, Wright LL, Zhou HQ.

J Med Chem. 2004 Jan 29;47(3):588-99.

PMID:
14736240
20.

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