Academic Journal
Microwave-assisted synthesis, characterization and cytotoxic studies of novel estrogen receptor alpha ligands towards human breast cancer cells
| العنوان: | Microwave-assisted synthesis, characterization and cytotoxic studies of novel estrogen receptor alpha ligands towards human breast cancer cells |
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| المؤلفون: | Bharathkumar, H., Mohan, C.D., Ananda, H., Li, F., Fuchs, J.E., Rangappa, S., Surender, M., Bulusu, K.C., Girish, K.S., Sethi, G., Bender, A., Basappab, ., Rangappa, K.S. |
| بيانات النشر: | Elsevier |
| سنة النشر: | 2015 |
| المجموعة: | ePrints@Bangalore University |
| مصطلحات موضوعية: | Chemistry |
| الوصف: | A new, simple, and microwave-assisted, solution-phase T3P (R)-DMSO mediated method for the preparation of a novel class of estrogen receptor alpha (ER alpha) ligands based on the 2-phenylquinoline scaffold was developed. Furthermore, the novel ER alpha ligands were tested for their bioactivity against ER alpha-positive and ER alpha-negative cell lines. The ligand (entry 4), with amine and nitro group substitution at C4 position, displayed significant cytotoxicity against MCF-7 and HepG2 cells with an IC50 value of 6 and 11 mu M, respectively. On the other hand, ER alpha-negative cells displayed resistance to quinolines induced cytotoxicity with an IC50 value >100 Mm and they does not induce cytotoxicity in normal breast epithelial cells. Molecular docking analyses suggest a consistent binding mode for these ER alpha ligands in the ligand binding domain of the human ER alpha and predict the ligands to occupy the hydrophobic cavity in a similar fashion as estradiol or GW2368. (C) 2015 Elsevier Ltd. All rights reserved. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | text |
| اللغة: | English |
| Relation: | http://eprints-bangaloreuniversity.in/6934/1/bharath%20kumar.pdf; Bharathkumar, H. and Mohan, C.D. and Ananda, H. and Li, F. and Fuchs, J.E. and Rangappa, S. and Surender, M. and Bulusu, K.C. and Girish, K.S. and Sethi, G. and Bender, A. and Basappab, . and Rangappa, K.S. (2015) Microwave-assisted synthesis, characterization and cytotoxic studies of novel estrogen receptor alpha ligands towards human breast cancer cells. Bioorganic and Medicinal Chemistry Letters, 25 (8). pp. 1804-1807. ISSN 0960-894X |
| الاتاحة: | http://eprints-bangaloreuniversity.in/6934/ http://eprints-bangaloreuniversity.in/6934/1/bharath%20kumar.pdf https://www.ncbi.nlm.nih.gov/pubmed/25797502 |
| رقم الانضمام: | edsbas.B15AE7F5 |
| قاعدة البيانات: | BASE |
| الوصف غير متاح. |