Title:Dual Aromatase-Sulphatase Inhibitors (DASIs) for the Treatment of
Hormone Dependent Breast Cancer
Volume: 21
Issue: 20
Author(s): Laxmi Banjare, Akhlesh Kumar Jain and Suresh Thareja*
Affiliation:
- Department of
Pharmaceutical, Sciences and Natural Products, Central University of Punjab, Bathinda, Punjab 151001, India
Keywords:
Hormone-dependent breast cancer, estrogen, anticancer agents, aromatase inhibitors, sulphatase inhibitors, dual inhibitors.
Abstract: Abstract: Breast cancer is the most frequently diagnosed cancer in women and the second most
common form of cancer, causing death after lung cancer, all across the globe at an alarming rate. The
level of estrogens in breast cancer tissues of postmenopausal women is 10-40 folds higher than the
non-carcinogenic breast tissues. As a result of this greater level of estrogen, breast tissue becomes
more prone to develop breast cancer; mainly, estradiol plays a significant role in the initiation and development
of hormone-dependent breast cancer. Androstenedione, Adrenal dehydroepiandrosterone
sulfate, and estrone-sulfate also play an important role as precursors for estrogen biosynthesis. Estrogen
deprivation exhibits an attractive phenomenon in the advancement of ideal therapeutics for the
treatment of breast cancer. Inhibition of aromatase and sulphatase emerged as an attractive therapy for
the treatment of hormone-dependent breast cancer via deprivation of estrogen by different pathways.
The cocktail of aromatase and sulphatase inhibitors known as Dual Aromatase-sulphatase Inhibitors
(DASIs) emerged as an attractive approach for effective estrogen deprivation. The present review article
focused on the journey of dual aromatase-sulphatase inhibitors from the beginning to date (2020).
Keeping in view the key observations, this review may be helpful for medicinal chemists to design
and develop new and efficient dual aromatase-sulphatase inhibitors for the possible treatment of hormone-
related breast cancer.