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Hormony steroidowe, leki przeciwzapalne, pigułki antykoncepcyjne. związki i ludzie : notatki historyczne (część 1 i 2)

Wicha Jerzy

Wiadomości Chemiczne

2021

[Z] 75, 5-6

677--753

A short historical outlook of steroid hormones isolation, structure elucidation and hormonal drugs development following by a survey of contraceptive therapeutics syntheses and advancements is given. Structural evolution of the first pills, “the pill”, to the presently used oral contraceptives for women is scrutinized. Comments on activities of selected major researchers in the field: Josef Fried, Russell E. Marker, Arthur J. Birch, Carl Djerassi, Georgy G. Pincus, M. C. Chang, John Rock, Igor V. Torgov, Zoltan G. Hajos and Herchel Smith from the personal prospect are presented. Steroid sex hormones, estrogens (female), androgens (male) and gestagens (progesterone, pregnancy hormone) were isolated and identified as chemical entities in 20-tiest and 30-ties of the 20th century. Development of partial synthesis of basic hormones from cholesterol made possible the initial steroid drugs production: Testosterone propionate and 17a-Methyltestosterone (Ciba) as well as Proviron, Progynon, Proluton (Schering AG). In 1940th and 1950th corticosteroids were isolated and recognized as “magic” anti-inflammatory and antiarthritic drugs. Growing demand for antiarthritic drugs in 1950th stimulated search for new corticosteroid analogues and new steroid row materials. Exploration of Mexican plant Dioscorea “cabeza” by Synthex SA provided economical starting material, diosgenin, and opened the new prospects for hormonal drug research and the production. Subsequently, highly active corticosteroid analogues were developed by several pharmaceutical companies and 19-norprogesterone analogues of high gestagenic activity were synthesized - Norethisterone (Synthex) and Norethyndrel (Searle). Complex studies on the application of Norethyndrel as oral contraceptive for women were carried out in the Worcester Foundation for Experimental Biology. In 1959 the first drug “the pill”, which was developed on the grounds of Searls’ Norethyndrel - Enovid was registered by Food and Drug Administration in the USA. Shortly after that Norlutin, based upon Synthex’s Norethisterone, had also been approved for application. Commercial success of “the pill”, Enovid and Norlutin, triggered a broad research aimed at the partial synthesis and application of related progesterone analogues. In the end of 1950th and the beginning of 1960th the total synthesis of estrogens and 19-norsteroids gained practical importance. On these grounds Norgestrel and its active enancjomer Levonorgestrel were developed and commercialized by Wyeth Laboratories Inc. in the USA as the first contraceptive products by total synthesis. Starting from 1970th medicinal applications of corticosteroids gradually diminished, whereas growing attention was given to the development of hormonal contraceptives suitable for general application. Several synthetic modifications of Norethisterone and Levonorgestrel were developed and produced in a large scale. Another class of oral contraceptives stem from the steroid total synthesis developed in the Russell Uclaf laboratories. Structurally these compounds are characterized by 19-norsteroid core and the presence of bulky substituent at the position 11ß, as 4-(N,N-dimethylamino)phenyl- in Mifepristone (RU 486). The synthesis of 19-norpregnane derivatives bearing at the position 11ß various large aromatic or alphatic groups, which currently is receiving a great deal of attention, is considered.