Tomczuk B - Search Results

1

Design, synthesis, and biological evaluation of novel potent and selective alphavbeta3/alphavbeta5 integrin dual inhibitors with improved bioavailability. Selection of the molecular core.

Marugán JJ, Manthey C, Anaclerio B, Lafrance L, Lu T, Markotan T, Leonard KA, Crysler C, Eisennagel S, Dasgupta M, Tomczuk B. Marugán JJ, et al. Among authors: tomczuk b. J Med Chem. 2005 Feb 24;48(4):926-34. doi: 10.1021/jm049725u. J Med Chem. 2005. PMID: 15715463

2

Non-peptidic alpha(v)beta3 antagonists containing indol-1-yl propionic acids.

Leonard K, Pan W, Anaclerio B, Gushue JM, Guo Z, DesJarlais RL, Chaikin MA, Lattanze J, Crysler C, Manthey CL, Tomczuk BE, Marugan JJ. Leonard K, et al. Among authors: tomczuk be. Bioorg Med Chem Lett. 2005 May 16;15(10):2679-84. doi: 10.1016/j.bmcl.2005.01.028. Bioorg Med Chem Lett. 2005. PMID: 15863341

3

Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.

Qiao L, Baumann CA, Crysler CS, Ninan NS, Abad MC, Spurlino JC, Desjarlais RL, Kervinen J, Neeper MP, Bayoumy SS, Williams R, Deckman IC, Dasgupta M, Reed RL, Huebert ND, Tomczuk BE, Moriarty KJ. Qiao L, et al. Bioorg Med Chem Lett. 2006 Jan 1;16(1):123-8. doi: 10.1016/j.bmcl.2005.09.037. Epub 2005 Oct 19. Bioorg Med Chem Lett. 2006. PMID: 16236500

4

A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.

Subasinghe NL, Travins JM, Ali F, Huang H, Ballentine SK, Marugán JJ, Khalil E, Hufnagel HR, Bone RF, DesJarlais RL, Crysler CS, Ninan N, Cummings MD, Molloy CJ, Tomczuk BE. Subasinghe NL, et al. Bioorg Med Chem Lett. 2006 Apr 15;16(8):2200-4. doi: 10.1016/j.bmcl.2006.01.036. Epub 2006 Feb 3. Bioorg Med Chem Lett. 2006. PMID: 16460935

5

Novel potent and selective alphavbeta3/alphavbeta5 integrin dual antagonists with reduced binding affinity for human serum albumin.

Raboisson P, Manthey CL, Chaikin M, Lattanze J, Crysler C, Leonard K, Pan W, Tomczuk BE, Marugán JJ. Raboisson P, et al. Eur J Med Chem. 2006 Jul;41(7):847-61. doi: 10.1016/j.ejmech.2006.03.008. Epub 2006 May 11. Eur J Med Chem. 2006. PMID: 16697080

6

Identification of novel short chain 4-substituted indoles as potent alphavbeta3 antagonist using structure-based drug design.

Raboisson P, Desjarlais RL, Reed R, Lattanze J, Chaikin M, Manthey CL, Tomczuk BE, Marugán JJ. Raboisson P, et al. Eur J Med Chem. 2007 Mar;42(3):334-43. doi: 10.1016/j.ejmech.2006.10.015. Epub 2006 Dec 20. Eur J Med Chem. 2007. PMID: 17184884

7

Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.

Kreutter KD, Lu T, Lee L, Giardino EC, Patel S, Huang H, Xu G, Fitzgerald M, Haertlein BJ, Mohan V, Crysler C, Eisennagel S, Dasgupta M, McMillan M, Spurlino JC, Huebert ND, Maryanoff BE, Tomczuk BE, Damiano BP, Player MR. Kreutter KD, et al. Bioorg Med Chem Lett. 2008 May 1;18(9):2865-70. doi: 10.1016/j.bmcl.2008.03.087. Epub 2008 Apr 8. Bioorg Med Chem Lett. 2008. PMID: 18420408

8

Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.

Tomczuk B, Lu T, Soll RM, Fedde C, Wang A, Murphy L, Crysler C, Dasgupta M, Eisennagel S, Spurlino J, Bone R. Tomczuk B, et al. Bioorg Med Chem Lett. 2003 Apr 17;13(8):1495-8. doi: 10.1016/s0960-894x(03)00125-2. Bioorg Med Chem Lett. 2003. PMID: 12668020

9

Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis.

Lu T, Markotan T, Coppo F, Tomczuk B, Crysler C, Eisennagel S, Spurlino J, Gremminger L, Soll RM, Giardino EC, Bone R. Lu T, et al. Among authors: tomczuk b. Bioorg Med Chem Lett. 2004 Jul 16;14(14):3727-31. doi: 10.1016/j.bmcl.2004.05.002. Bioorg Med Chem Lett. 2004. PMID: 15203151

10

2-(2-Chloro-6-fluorophenyl)acetamides as potent thrombin inhibitors.

Lee L, Kreutter KD, Pan W, Crysler C, Spurlino J, Player MR, Tomczuk B, Lu T. Lee L, et al. Among authors: tomczuk b. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6266-9. doi: 10.1016/j.bmcl.2007.09.013. Epub 2007 Sep 8. Bioorg Med Chem Lett. 2007. PMID: 17889527

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