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Chapter: Medicinal Chemistry : Steroids

Oestrogens : i. Oestradiol derivatives ii. Diethylstilbestrol (Stilbetin, Stilphstrol) iii. Dienestrol (Estragard)

Steroids - Drugs Acting on Endocrine System


The mammalian ovary is a source of steroid hormones that maintain reproductive functions and oestrogen secretion in females.



Oestrogens could be classified as follows:

i.            Natural steroidal: Oestradiol, Oesterone

ii.          Synthetic steroidal: Ethynyl oestradiol, Mestranol

iii.        Nonsteroidal synthetic: Stilbesterol


i. Oestradiol derivatives

Oestradiol Derivatives

Properties: It exists as a creamy white crystalline powder hygroscopic, insoluble in water and soluble in alcohol.


ii. Diethylstilbestrol (Stilbetin, Stilphstrol)

Properties: It is a white crystalline powder, insoluble in water and soluble in alcohol.

Dose: The dose for menopausal symptoms orally is 0.1–2 mg. For secondary amenorrhoea, the dose is 0.2–0.5 mg and for carcinoma, of the prostate the intake is 3 mg per day.


Method-I From: Anisaldehyde (Dodds method)

Method-II From: Anethole


iii. Dienestrol (Estragard)


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