Steroidal Anticancer Agents: An Overview of Estradiol-related Compounds

Abstract

Research of steroidal compounds as anticancer agents started almost 50 years ago. During the past decades, several innovative new steroids, like cyproterone, finasteride, estramustin, exemestane and fulvestrant have successfully become a part of routine clinical practice. Meanwhile, a vast amount of new information have accumulated about the functions of the endogenous steroid system (including the characterization of enzymes, receptors, transcription pathways, etc.) and about the role of steroids in carcinogenesis. Therefore, it is regularly required to review the latest published results, focusing on a well-defined part within this research field that has definitely developed into a highly diversified speciality by now. Herein, we make an attempt to summarize the most recent results reported about anticancer agents of estrane backbone, focusing on their mechanisms of action and their structure-activity relationships. Due to the vast number and various accessibilities of scientific publications, neither other reviews nor this one can be considered as absolutely exhaustive. In spite of these restrictive factors, the current review makes a good opportunity to define the recent scientific trends in the field of estradiol-related anticancer agents.

Anticancer effects and the mechanism underlying 2‑methoxyestradiol in human osteosarcoma <em>in&nbsp;vitro</em> and <em>in&nbsp;vivo</em>

“…2-ME induced both endogenous and exogenous apoptotic pathways in the present study, this may explain the broad-spectrum activity of 2-ME and the effects of 2-ME on a variety of cellular processes, including microtubule destruction, initiation of signal transduction pathways and production of reactive oxygen species, ultimately inducing apoptosis ( 37 ). Flow cytometry and TUNEL staining were used in the present study to detect apoptosis of tumor cells and xenograft tumor tissues, respectively.…”

Whole-genome and enzymatic analyses of an androstenedione-producing Mycobacterium strain with residual phytosterol-degrading pathways

“…Among the aforementioned three important androstane steroids, 4-AD is one of the most important starting materials [ 28 ] in the synthesis of steroid medicines such as abiraterone [ 29 ], testosterone [ 30 ], estradiol [ 31 ] and progesterone [ 32 ]. Microbial bioconversion of phytosterols to 4-AD is still an industrial challenge.…”

Effect of morphology and support of copper nanoparticles on basic ovarian granulosa cell functions

“…Moreover, the potential utility of the stimulatory properties of CuNPs for the improvement of reproductive processes cannot be overruled. However, it must be taken into account that the stimulatory properties of CuNPs resemble some signs of malignant transformation of ovarian cells, which are characterized just by these changes (Minorics and Zupko, 2018;Sharma et al, 2019). Therefore, the efficiency of CuNPs to induce such transformations should be carefully checked before application.…”