Main chain and side chain chiral methylated somatostatin analogs: Syntheses and conformational analyses

…, YB He, K Raynor, M Tallent, T Reisine…

Index: Huang, Ziwei; He, Ya-Bo; Raynor, Karen; Tallent, Melanie; Reisine, Terry; Goodman, Murray Journal of the American Chemical Society, 1992 , vol. 114, # 24 p. 9390 - 9401

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Citation Number: 133

Abstract

Abstract: We have developed an integrated approach for investigating the'bioactive conformations" of the main chain and side chains for the somatostatin analog~[Pro~-Phe~-~- Trp~-Lys~-Thr~~-Phe'~]. A series of analogs have been synthesized incorporating a- methylated and 8-methylated residues at positions 7, 8, and 11. These analogs display dramatic differences in in vitro binding affinities for somatostatin receptors. Using 500-MHz ...