دورية أكاديمية
Role of Natural and Synthetic Flavonoids as Potential Aromatase Inhibitors in Breast Cancer: Structure-Activity Relationship Perspective.
| العنوان: | Role of Natural and Synthetic Flavonoids as Potential Aromatase Inhibitors in Breast Cancer: Structure-Activity Relationship Perspective. |
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| المؤلفون: | Shah U; Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology (CHARUSAT), CHARUSAT Campus, Changa 388421, India., Patel A; Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology (CHARUSAT), CHARUSAT Campus, Changa 388421, India., Patel S; Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology (CHARUSAT), CHARUSAT Campus, Changa 388421, India., Patel M; Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology (CHARUSAT), CHARUSAT Campus, Changa 388421, India., Patel A; Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology (CHARUSAT), CHARUSAT Campus, Changa 388421, India., Patel S; Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology (CHARUSAT), CHARUSAT Campus, Changa 388421, India., Patel S; Department of Pharmacology, L.M. College of Pharmacy, Ahmedabad, Gujarat, India., Maheshwari R; Department of Pharmacy, Sumandeep Vidyapeeth, Piparia, Waghodiya, Vadodara, Gujarat, India., Mtewa AG; Chemistry Section, Institute of Technology, Malawi University of Science and Technology, Thyolo, Malawi., Gandhi K; Department of Chemistry, University of Manitoba, Winnipeg, Manitoba R3T 2N2, Canada. |
| المصدر: | Anti-cancer agents in medicinal chemistry [Anticancer Agents Med Chem] 2022; Vol. 22 (11), pp. 2063-2079. |
| نوع المنشور: | Journal Article; Review |
| اللغة: | English |
| بيانات الدورية: | Publisher: Bentham Science Publishers Country of Publication: Netherlands NLM ID: 101265649 Publication Model: Print Cited Medium: Internet ISSN: 1875-5992 (Electronic) Linking ISSN: 18715206 NLM ISO Abbreviation: Anticancer Agents Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Amsterdam : Bentham Science Publishers Original Publication: Sharjah, U.A.E. ; San Francisco, CA : Bentham Science Publishers, [2006]- |
| مواضيع طبية MeSH: | Breast Neoplasms*/drug therapy , Breast Neoplasms*/metabolism , Flavones*, Aromatase/metabolism ; Aromatase Inhibitors/chemistry ; Estrogens ; Female ; Flavonoids/pharmacology ; Flavonoids/therapeutic use ; Humans ; Structure-Activity Relationship |
| مستخلص: | World Health Organization categorized breast cancer as one of the leading cancer types in females worldwide, and its treatment remains challenging. Accumulated evidence suggested the role of estrogen and its metabolites in pre- and post-menopausal women. Upregulation of estrogen-dependent aromatase is significantly involved in the pathogenesis of breast cancer. Several aromatase inhibitors, such as exemestane, formestane, and letrozole, are being used clinically, owing to their estrogen suppression role. Apart from these drugs, several other molecules, such as natural and synthetic flavonoids, have been reported widely for a similar biological activity. However, some reasonable modifications are required for these structures to achieve desired efficacy and to alleviate toxicity. Designing a novel aromatase inhibitor will be possible if we can establish a rational correlation between the chemistry and biological features of the existing molecules. The benzopyranone- ring system, present in the flavonoid molecules, has been reported as a pharmacophore due to its inhibitory activity on aromatase, which helps repress breast cancer progression. This essential feature has been utilized to modify several natural flavonoids into 5 and 7 hydroxy/methoxy flavone, 4-imidazolyl/triazolyl flavone, 5,4'- diamino flavone, 7,8- benzo-4-imidazolyl flavone, α-naphthoflavone, and 2-azole/thiazolyl isoflavone derivatives. These scaffolds have been considered in this review for meticulous study in aspects of the structure-activity relationship for aromatase inhibitory activity, and it would likely pave the way for designing a potential lead candidate in the future. (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.) |
| فهرسة مساهمة: | Keywords: CYP 450 enzyme inhibitors; Flavonoids; aromatase; breast cancer; chalcone; structure-activity relationship |
| المشرفين على المادة: | 0 (Aromatase Inhibitors) 0 (Estrogens) 0 (Flavones) 0 (Flavonoids) EC 1.14.14.1 (Aromatase) |
| تواريخ الأحداث: | Date Created: 20211027 Date Completed: 20220523 Latest Revision: 20220622 |
| رمز التحديث: | 20240628 |
| DOI: | 10.2174/1871520621666211026101252 |
| PMID: | 34702156 |
| قاعدة البيانات: | MEDLINE |
| تدمد: | 1875-5992 |
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| DOI: | 10.2174/1871520621666211026101252 |