Add time:08/08/2019         Source:sciencedirect.com

Publisher SummaryThis chapter discusses heterosteroids and drug research. Heterosteroids may have heteroatoms as part of the steroid nucleus, or the heteroatoms may be extranuclear, forming part of a fused or spiro ring system, an attached group, or a side-chain. A relatively recent approach to new drug development is the design of inhibitors of steroid hormone biosynthesis. Such agents may be more selective in their actions. The suicide substrates and the pseudo-irreversible or very tight binding inhibitors may be more promising in achieving selectivity. Suicide substrates are inocuous until transformed by their target enzyme into highly reactive alkylating groups. Certain heterosteroids have proved to be active in inhibiting some steroid biosynthetic enzymes. An account of such heterosteroids is given under the headings: aromatase inhibitors, 5α-reductase inhibitors, and 3β-hydroxysteroid dehydrogenase inhibitors. Earlier, under mifepristone and danazol, mention was made of inhibitory activity of the drugs on some enzymes. Aromatase (oestrogen synthetase) inhibitors, by suppressing the oestrogen biosynthesis, can have potential use in the treatment of oestrogen-dependent mammary carcinoma and even benign prostatic hyperplasia.

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