Browsing by Author "Das, Sweety"

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    Medicinal chemistry aspects and synthetic strategies of coumarin as aromatase inhibitors: an overview
    (Springer, 2022-12-05T00:00:00) Ratre, Pooja; Kulkarni, Swanand; Das, Sweety; Liang, Chengyuan; Mishra, Pradyumna Kumar; Thareja, Suresh
    Coumarin is a bicyclic oxygen bearing heterocyclic scaffold formed by fusion of benzene with the pyrone ring. Because of its unique physicochemical characteristics and the ease with which it may be transformed into a wide range of functionalized coumarins during�synthesis, coumarin provides a privileged scaffold for medicinal chemists. As a result, many coumarin derivatives have been developed, synthesized, and evaluated to target a variety of therapeutic domains, thereby making it an attractive template for designing novel anti-breast cancer compounds. The main culprit in estrogen overproduction in the estrogen-dependent breast cancer (EDBC), is the enzyme aromatase (AR), and it is thought to be a significant target for the effective treatment of EDBC. Considering coumarins versatility, this review presents a detailed overview of diverse study of aromatase as a target for coumarins. An overview of structure�activity relationship analysis of coumarin core is also included so as to summarize the desired pharmacophoric features essential for design and development of aromatase inhibitors (AIs) using coumarin core. Identification of key synthesis techniques that could aid researchers in designing and developing novel analogues with significant anti-breast cancer properties along with their mechanism of action have also been covered in the current review. Graphical Abstract: [Figure not available: see fulltext.] � 2022, The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.
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    Selective Estrogen Receptor Modulators (SERMs) for the treatment of ER+ breast cancer: An overview
    (Elsevier B.V., 2022-08-02T00:00:00) Das, Sweety; Kulkarni, Swanand; Singh, Yogesh; Kumar, Pradeep; Thareja, Suresh
    Breast cancer is a major threat to women's lives throughout the world. Hormone-dependent or estrogen-receptor positive (ER+) breast cancer accounts for more than 80% of all instances. Selective Estrogen Receptor Modulators (SERMs), which specifically control the ERs and limit the progression of breast malignancy, have drawn the interest of researchers in the treatment of breast cancer by regulation of the estrogen receptors (ER), particularly ER?. The mode of action, anti-proliferative potential, SAR, and favourable interactions of the potent candidates are elaborated. Many potent SERMs with diversity in structural space have been rationally designed and reported in the literature for their anti-breast cancer activity. These SERMs exhibited remarkable anti-proliferative activity against ER+ BC. Since, ER? is responsible for the initiation and progression of BC, there is an urgent need to strategically design and synthesize new SERMs, having more selective binding towards ER?. Long term use of traditionally marketed SERMs is associated with several adverse effects, such as development of endometrial cancer and other disorders. Insight of structural features in the present review will prove to be a guideline for the researchers to design and develop potent SERMs for the treatment of ER+ breast cancer. � 2022 Elsevier B.V.