Structure-toxicity relationships of the tetramethylated tetralin and indane analogs of retinoic acid

Teratology. 1987 Dec;36(3):303-11. doi: 10.1002/tera.1420360306.

Abstract

The teratogenicity of retinoids containing either tetramethylated tetralin (Ro 13-6307 or Ro 13-2389) or tetramethylated indane (Ro 13-4306) ring system substitutions was compared to the teratogenic potency of all-trans-retinoic acid. Single oral doses, administered to Syrian Golden hamsters at 10:00 A.M. on day 8 of gestation, induced a syndrome of malformations identical to that induced by treatment with all-trans-retinoic acid. These retinoids failed to induce signs of maternal hypervitaminosis A at doses associated with a significant teratogenic response. The tetramethylated tetralin retinoids and indane retinoid were 18 and 2.4 times as embryotoxic on a molar basis, respectively, as all-trans-retinoic acid. Introduction of a supplementary ring in the side-chain restricted polyene chain flexibility and maintained the hydrophobic plane of the chain. The present results are consistent with previous studies showing that the presence of or biotransformation to a free acid congener was necessary for retinoid teratogenic activity in hamsters and that increasing conformational restriction of acidic retinoids increased teratogenic potency.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Abnormalities, Drug-Induced*
  • Animals
  • Cricetinae
  • Female
  • Indans / toxicity*
  • Indenes / toxicity*
  • Mesocricetus
  • Naphthalenes / toxicity*
  • Pregnancy
  • Structure-Activity Relationship
  • Syndrome
  • Teratogens*
  • Tetrahydronaphthalenes / toxicity*
  • Tretinoin / analogs & derivatives*
  • Tretinoin / toxicity*

Substances

  • Indans
  • Indenes
  • Naphthalenes
  • Teratogens
  • Tetrahydronaphthalenes
  • Tretinoin