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A peptide-doxorubicin 'prodrug' activated by prostate-specific antigen selectively kills prostate tumor cells positive for prostate-specific antigen in vivo.
DeFeo-Jones D, Garsky VM, Wong BK, Feng DM, Bolyar T, Haskell K, Kiefer DM, Leander K, McAvoy E, Lumma P, Wai J, Senderak ET, Motzel SL, Keenan K, Van Zwieten M, Lin JH, Freidinger R, Huff J, Oliff A, Jones RE. DeFeo-Jones D, et al. Nat Med. 2000 Nov;6(11):1248-52. doi: 10.1038/81351. Nat Med. 2000. PMID: 11062536
2,3-diaminopyridine bradykinin B1 receptor antagonists.
Kuduk SD, Ng C, Feng DM, Wai JM, Chang RS, Harrell CM, Murphy KL, Ransom RW, Reiss D, Ivarsson M, Mason G, Boyce S, Tang C, Prueksaritanont T, Freidinger RM, Pettibone DJ, Bock MG. Kuduk SD, et al. Among authors: freidinger rm. J Med Chem. 2004 Dec 16;47(26):6439-42. doi: 10.1021/jm049394l. J Med Chem. 2004. PMID: 15588075
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.
Williams PD, Clineschmidt BV, Erb JM, Freidinger RM, Guidotti MT, Lis EV, Pawluczyk JM, Pettibone DJ, Reiss DR, Veber DF, et al. Williams PD, et al. Among authors: freidinger rm. J Med Chem. 1995 Nov 10;38(23):4634-6. doi: 10.1021/jm00023a002. J Med Chem. 1995. PMID: 7473590 No abstract available.
Conformationally constrained o-tolylpiperazine camphorsulfonamide oxytocin antagonists. Structural modifications that provide high receptor affinity and suggest a bioactive conformation.
Williams PD, Ball RG, Clineschmidt BV, Culberson JC, Erb JM, Freidinger RM, Pawluczyk JM, Perlow DS, Pettibone DJ, Veber DF. Williams PD, et al. Among authors: freidinger rm. Bioorg Med Chem. 1994 Sep;2(9):971-85. doi: 10.1016/s0968-0896(00)82046-5. Bioorg Med Chem. 1994. PMID: 7712132
84 results