具有生理活性的甾体酰胺类化合物

在甾体的甾核或支链上引入不同的官能团后可得到不同生理活性的化合物,它们有可能会成为人类治疗不同疾病的药物,因此甾体药物除了作为传统激素类药物使用外,在抗肿瘤药物、抗炎药物中的应用也成为甾体的重要研究内容之一。含有酰胺官能团的甾体化合物具有很好的生物活性。本文按照酰胺基团在甾体酰胺化合物中的位置进行分类,同时结合本课题组在甾体酰胺化合物的合成和生理活性研究方面所取得的一些成果,概述了近几年来新合成及发现的甾体酰胺类化合物及其衍生物的生理活性及研究进展,包括作为抗肿瘤药物的甾体酰胺化合物的设计、筛选、对5α-还原酶的抑制作用、抑制肿瘤细胞生长增殖活性及抗菌作用,并对此方面的发展趋势、应用前景作了展望。

Steroidal Amides with Biological Activities

The compounds with different bioactivities are obtained when some different functional groups are introduced into a nucleus or side chain of a steroid and they may become new drugs to treat different diseases.Besides applying to hormonal drugs,some steroidal compounds have exhibited a broad spectrum of biologic activities,such as antibacterium,inhibition of 5α-reductase and anti-tumor activities.Some modified steroidal compounds,such as steroidal amides that contain —NHCO— group,exhibit valuable biological activities and become an important research field of steroidal medicinal chemistry.Combined with our investigation,the studies on biological and physiological functions of the steroidal amides in recent years have been reviewed according to the location of different substituent groups on steroid,including the design and screening of the steroidal amides as cytotoxic agents,5α-reductase inhibitors and antibiotics.