C32-O-phenalkyl ether derivatives of the immunosuppressant ascomycin: a tether length study

  • Bioorg Med Chem Lett. 1999 Jul 19;9(14):2085-8. doi: 10.1016/s0960-894x(99)00335-2.
M T Goulet  1 ,  P J Sinclair ,  F Wong ,  M J Staruch ,  F J Dumont ,  J G Cryan ,  G J Wiederrecht ,  M J Wyvratt ,  W H Parsons
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
PMID: 10450986 DOI: 10.1016/s0960-894x(99)00335-2
Abstract

A tether length study of C32-O-phenalkyl ether derivatives of ascomycin was conducted wherein it was determined that a 2-carbon tether provides optimum in vitro immunosuppressive activity. Oxygen-bearing substituents along the 2-carbon tether can further increase the potency of this design.