Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer

• Published in: European journal of medicinal chemistry Vol. 105; pp. 1 - 38
• Main Authors: Yadav, Mange Ram, Barmade, Mahesh A., Tamboli, Riyaj S., Murumkar, Prashant R.
• Format: Journal Article
• Language: English
• Published: France Elsevier Masson SAS 13-11-2015
• Subjects: Aromatase - metabolism; Aromatase inhibitors; Aromatase Inhibitors - chemical synthesis; Aromatase Inhibitors - chemistry; Aromatase Inhibitors - pharmacology; Breast cancer; Breast Neoplasms - drug therapy; Breast Neoplasms - enzymology; Drug Design; Female; Humans; Medicinal chemistry; Models, Molecular; Molecular modeling; Molecular Structure; Ring substituted androstanes; Steroids; Medicinal chemistry; Breast cancer; Molecular modeling; Ring substituted androstanes; Aromatase inhibitors; Steroids
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2015.09.038

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.
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•The review provides extensive literature on steroidal aromatase inhibitors.•Steroidal aromatase inhibitors have been classified on the basis of their ring modifications.•Review is helpful for development of novel steroidal aromatase inhibitors for the treatment of breast cancer.•Importance of different substituents on A/B/D rings has been discussed with concluding remarks.