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Convergent, parallel synthesis of a series of beta-substituted 1,2,4-oxadiazole butanoic acids as potent and selective alpha(v)beta3 receptor antagonists.
Boys ML, Schretzman LA, Chandrakumar NS, Tollefson MB, Mohler SB, Downs VL, Penning TD, Russell MA, Wendt JA, Chen BB, Stenmark HG, Wu H, Spangler DP, Clare M, Desai BN, Khanna IK, Nguyen MN, Duffin T, Engleman VW, Finn MB, Freeman SK, Hanneke ML, Keene JL, Klover JA, Nickols GA, Nickols MA, Steininger CN, Westlin M, Westlin W, Yu YX, Wang Y, Dalton CR, Norring SA. Boys ML, et al. Among authors: freeman sk. Bioorg Med Chem Lett. 2006 Feb 15;16(4):839-44. doi: 10.1016/j.bmcl.2005.11.008. Epub 2005 Nov 17. Bioorg Med Chem Lett. 2006. PMID: 16298127
R-isomers of Arg-Gly-Asp (RGD) mimics as potent alphavbeta3 inhibitors.
Nagarajan SR, Devadas B, Malecha JW, Lu HF, Ruminski PG, Rico JG, Rogers TE, Marrufo LD, Collins JT, Kleine HP, Lantz MK, Zhu J, Green NF, Russell MA, Landis BH, Miller LM, Meyer DM, Duffin TD, Engleman VW, Finn MB, Freeman SK, Griggs DW, Williams ML, Nickols MA, Pegg JA, Shannon KE, Steininger C, Westlin MM, Nickols GA, Keene JL. Nagarajan SR, et al. Among authors: freeman sk. Bioorg Med Chem. 2007 Jun 1;15(11):3783-800. doi: 10.1016/j.bmc.2007.03.034. Epub 2007 Mar 15. Bioorg Med Chem. 2007. PMID: 17399986
Synthesis of cinnamic acids and related isosteres as potent and selective alpha v beta 3 receptor antagonists.
Penning TD, Russell MA, Chen BB, Chen HY, Desai BN, Docter SH, Edwards DJ, Gesicki GJ, Liang CD, Malecha JW, Yu SS, Engleman VW, Freeman SK, Hanneke ML, Shannon KE, Westlin MM, Nickols GA. Penning TD, et al. Among authors: freeman sk. Bioorg Med Chem Lett. 2004 Mar 22;14(6):1471-6. doi: 10.1016/j.bmcl.2004.01.015. Bioorg Med Chem Lett. 2004. PMID: 15006384
Synthesis of 2,5-thiazole butanoic acids as potent and selective alpha(v)beta3 integrin receptor antagonists with improved oral pharmacokinetic properties.
Wendt JA, Wu H, Stenmark HG, Boys ML, Downs VL, Penning TD, Chen BB, Wang Y, Duffin T, Finn MB, Keene JL, Engleman VW, Freeman SK, Hanneke ML, Shannon KE, Nickols MA, Steininger CN, Westlin M, Klover JA, Westlin W, Nickols GA, Russell MA. Wendt JA, et al. Among authors: freeman sk. Bioorg Med Chem Lett. 2006 Feb 15;16(4):845-9. doi: 10.1016/j.bmcl.2005.11.017. Epub 2005 Nov 21. Bioorg Med Chem Lett. 2006. PMID: 16303301
Synthesis of pyrazoles and isoxazoles as potent alpha(v)beta3 receptor antagonists.
Penning TD, Khilevich A, Chen BB, Russell MA, Boys ML, Wang Y, Duffin T, Engleman VW, Finn MB, Freeman SK, Hanneke ML, Keene JL, Klover JA, Nickols GA, Nickols MA, Rader RK, Settle SL, Shannon KE, Steininger CN, Westlin MM, Westlin WF. Penning TD, et al. Among authors: freeman sk. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3156-61. doi: 10.1016/j.bmcl.2006.03.045. Epub 2006 Apr 18. Bioorg Med Chem Lett. 2006. PMID: 16621534
Discovery of +(2-{4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acid as potent and selective alphavbeta3 inhibitor: design, synthesis, and optimization.
Nagarajan SR, Lu HF, Gasiecki AF, Khanna IK, Parikh MD, Desai BN, Rogers TE, Clare M, Chen BB, Russell MA, Keene JL, Duffin T, Engleman VW, Finn MB, Freeman SK, Klover JA, Nickols GA, Nickols MA, Shannon KE, Steininger CA, Westlin WF, Westlin MM, Williams ML. Nagarajan SR, et al. Among authors: freeman sk. Bioorg Med Chem. 2007 May 15;15(10):3390-412. doi: 10.1016/j.bmc.2007.03.020. Epub 2007 Mar 13. Bioorg Med Chem. 2007. PMID: 17387018
Design and synthesis of novel imidazole-substituted dipeptide amides as potent and selective inhibitors of Candida albicans myristoylCoA:protein N-myristoyltransferase and identification of related tripeptide inhibitors with mechanism-based antifungal activity.
Devadas B, Freeman SK, Zupec ME, Lu HF, Nagarajan SR, Kishore NS, Lodge JK, Kuneman DW, McWherter CA, Vinjamoori DV, Getman DP, Gordon JI, Sikorski JA. Devadas B, et al. Among authors: freeman sk. J Med Chem. 1997 Aug 1;40(16):2609-25. doi: 10.1021/jm970094w. J Med Chem. 1997. PMID: 9258368
40 results