Pharmacy Department, Faculty of Tech. and Engg., The M. S. University of Baroda, Vadodara 390 001, Gujarat, India.
Pharmacy Department, Faculty of Tech. and Engg., The M. S. University of Baroda, Vadodara 390 001, Gujarat, India.
Eur J Med Chem. 2015 Nov 13;105:1-38. doi: 10.1016/j.ejmech.2015.09.038. Epub 2015 Oct 3.
Breast cancer, an emerging disease among the women population, occurs due to overexpression of estrogens. The enzyme aromatase plays a key rate limiting role in the biosynthesis of estrogens. Certain clinical advantages of the use of exemestane, a steroidal aromatase inhibitor over non-steroidal aromatase inhibitors have drawn the attention of researchers for the development of novel steroidal aromatase inhibitors.The current review is a humble attempt to compile the reports by various researchers till date on the synthesis of steroidal aromatase inhibitors. It has been tried to encompass the structural modifications carried out by various researchers in the steroid ring system by taking up the functional group modifications on rings A, B, ring A/B junction, ring-D, ring modifications, bridged derivatives and heterocyclic ring-fused derivatives in a systematic way.
乳腺癌是女性人群中新兴的疾病，它的发生是由于雌激素的过度表达。芳香酶在雌激素的生物合成中起着关键的限速作用。与非甾体类芳香酶抑制剂相比，甾体类芳香酶抑制剂依西美坦在某些临床方面具有优势，这引起了研究人员的关注，促使他们开发新型的甾体类芳香酶抑制剂。目前的综述是对迄今为止各种研究人员关于甾体类芳香酶抑制剂合成报告的一次尝试性汇编。我们试图通过系统地研究甾体环系统中各种研究人员进行的结构修饰，涵盖了在 A 环、B 环、A/B 环连接点、D 环、环修饰、桥接衍生物和杂环稠合衍生物上进行的官能团修饰。
