PharmaTutor (February- 2014)
ISSN: 2347 - 7881
Received On: 01/12/2013; Accepted On: 12/01/2014; Published On: 10/02/2014
Author: Vanraj Thakor1*, Jalpa Kher2, Fenil Bhayani1, Bhavini Atodaria1, Malleshappa Noolvi1
1Department of Pharmaceutical Chemistry,
Shree Dhanvantary college of pharmacy, Kim, Surat, Gujarat, India.
2 Ashok & Rita Patel institute of Biotechnology, New Vallabh Vidyanagar, Gujarat, India
*vanraj7777@gmail.com
ABSTRACT: Aromatase and 17-ßHSD inhibitors are main target of pharmacological interest for the treatment of estrogen dependent cancers. Chalcones, Coumarins, Flavones, Isoflavones have been reported for such inhibition and are used for treatment of breast tumors. So in this topic, Flavone derivatives containing Imidathiadiazole, Thiadiazole, Triazole and benzimidazole hetrocycles synthesised by using simple laboratory reagents like 2-Hydroxy Acetophenone and 4-Hydroxy Benzaldehyde to convert chalcone leads to formation of Flavones by cyclization using Microwave and followed by attachment of different hetrocycles to form Flavone derivatives and characterized by IR, 1H NMR, 13C NMR spectroscopy and elemental analysis. These Flavone derivatives found to exhibit moderate to high inhibitory activity against Estrogen dependent cancers.
How to cite this article: V Thakor, J Kher, F Bhayani, B Atodaria, M Noolvi, Synthesis and Anticancer activity of Flavone Derivatives against Estrogen Dependent Cancers by rational approach, PharmaTutor, 2014, 2(2), 33-43
[ABSTRACT WITH CITATION] [VIEW AS HTML]
REFERENCES:
1. Tortora Grabowski, “Principles of Anatomy & Physiology ”, 10th Edition”, Wiley International Publications, 2003, pp: 95-96.
2. National Cancer Institute; 2001. NIH Pub. No. 01-4969
cancer.gov/cancertopics/understandingcancer/estrogenreceptors/page5
3. Pradip singh et. al. Triazole Chalcone derivatives European Journal of Medicinal Chemistry, 2012, 47: 594-600.
4. Yanyan Hong, Shiuan Chen, Aromatase, estrone sulfatase, and 17-hydroxysteroid dehydrogenase: Structure–function studies and inhibitor development. Molecular and Cellular Endocrinology, 2011, 340: 120-126.
5. MedKoo product information: Acolbifene; EM-652, SCH-57068, CAS#182167-02-8 medKoo.com
6. Sandrine Marchais-Oberwinkler and Claudia Henn, 17-Hydroxysteroid dehydrogenases as therapeutic targets: Protein structures, functions, and recent progress in inhibitor development. Journal of Steroid Biochemistry & Molecular Biology, 2011, 125: 66–82.
7. Sampo Karkola, Academic Dissertation “Molecular Modelling of Estrogen producing enzyme CYP450 Aromatase and 17 β-Hydroxysteroid Dehydrogenase Type 1” University of Helsinki Finland 2009.
8. Pramod Kulkarni et. al. An eco friendly method for synthesis of Flavones. Chemistry Journal 2012, 2: 106-110.
9. Ramesh Kamboj et. al. An environmentally sound approach for synthesis of some Flavanone, International Journal of ChemTeach Research, 2011, 3: 901-910.
10. Christine Dyrager, PhD Thesis “Design and Synthesis of Chalcone and Chromone Derivatives as Novel Anticancer Agents” Department of Chemistry, University of Gothenburg 2012.
11. Kempegowda, Senthil Kumar G.P. et. al. Thiadiazole: Progress report on Biological activities, Der Pharma Chemica, 2011, 3: 330-341.
12. Rakesh Yadav, Divya Yadav and Sarvesh Kumar Paliwal; Novel Biphenyl Imidazo[2,1-b][1,3,4]-Thiadiazole -a versatile scaffold; International Journal of Pharmaceutical Sciences, 2012, 2: 1-18.