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PMID: 363444 Published · ppublish English Journal Article Review

Retinoids, a new class of compounds with prophylactic and therapeutic activities in oncology and dermatology.

Experientia ·Vol. 34 ·No. 9 ·1978-09-15 ·Pages 1105-19

Mayer H, Bollag W, Hänni R, Rüegg R

Abstract

A review of recent investigations in the retinoid field is presented. Retinoic acid exerts a prophylactic and a therapeutic effect on chemically induced benign and malignant epithelial tumors in mice. In clinical studies positive therapeutic results have been obtained in patients with preneoplastic and neoplastic epithelial lesions. However, treatment with retinoic acid is limited by serious side effects (hypervitaminosis A syndrome). Therefore, the synthesis of analogs of retinoic acid (retinoids) possessing a more favorable therapeutic ratio has been initiated. Among a large series of synthesized compounds, certain aromatic analogs proved to have a particularly favorable therapeutic ratio. The structure-activity relationship of the most active retinoids is discussed including some biological data concerning prophylaxis and therapy of epithelial tumors. The total synthesis of retinoids according to various building schemes is discussed in detail. Methods for the synthesis of the cyclic end group, of the polyene chain component, and of the full retinoid skeleton are described. Metabolic studies of retinoic acid and of the most active retinoid, as well as the synthesis of some isolated metabolites are outlined. Suggestions concerning the mechanism of action of retinoids are made. Some clinical results on the treatment of acne, psoriasis and precancerous conditions are reported.

MeSH Terms
Animals Carcinoma/drug therapy Humans Neoplasms, Experimental/drug therapy Papilloma/drug therapy Retinaldehyde/therapeutic use Skin Diseases/drug therapy,prevention & control Skin Neoplasms/drug therapy Structure-Activity Relationship Tretinoin/analogs & derivatives,metabolism,therapeutic use Vitamin A/adverse effects,analogs & derivatives,therapeutic use
Chemicals
Vitamin A Tretinoin Retinaldehyde
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Mayer H
Bollag W
Hänni R
Rüegg R
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76 references, click to expand
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Article Info
Journal
Experientia
Abbr.
Experientia
ISSN
0014-4754
DOI
10.1007/BF01922901
Published
1978-09-15
Pages
1105-19
Language
English
Region
Switzerland
NLM ID
0376547
Subset
IM
External Links
PubMed source DOI: 10.1007/BF01922901
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