Synthesis of pyrazole-substituted chromene analogues with selective anti-leukemic activity
- 作者: Madhu G.1, Sudhakar M.1, Santosh Kumar K.1, Rajashekher Reddy G.1, Sravani A.2, Ramakrishna K.2, Prasad Rao C.1
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隶属关系:
- Natural Products Laboratory, Department of Chemistry
- Molecular Medicine and Therapeutics Laboratory, Centre for Plant Molecular Biology
- 期: 卷 87, 编号 10 (2017)
- 页面: 2421-2428
- 栏目: Article
- URL: https://journals.rcsi.science/1070-3632/article/view/221466
- DOI: https://doi.org/10.1134/S1070363217100243
- ID: 221466
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详细
We report design and synthesis of a series of flavanone/chromene derivatives containing pyrazoles 6a–6h and 8a–8e with potent anti-leukemic activity. Anti-leukemic activity of novel flavanone derivatives was tested using the K562 cell line. The parental flavanone was selected as the reference compound in identification of analogues with superior anti-leukemic activity. More than two-thirds of the derivatives displayed higher activity than the initial flavanone. Positions of substituents that promoted anti-leukemic activity were identified on both the chromene and pyrazole fragments. Compounds 6b and 6c showed the highest activity against K562 cell line, with IC50 values 3.0 and 0.5 μM respectively. Notably, compounds 6b and 6c displayed very high selectivity in inhibition of leukemic cells (K562) but not of healthy HEK293 cells or solid cancer cell lines HeLa, MCF7 and BT474. Moreover, both the 6b and 6c compounds were predicted to have good ADME properties.
作者简介
G. Madhu
Natural Products Laboratory, Department of Chemistry
Email: prasadraoou@yahoo.com
印度, Hyderabad, Telangana, 500007
M. Sudhakar
Natural Products Laboratory, Department of Chemistry
Email: prasadraoou@yahoo.com
印度, Hyderabad, Telangana, 500007
K. Santosh Kumar
Natural Products Laboratory, Department of Chemistry
Email: prasadraoou@yahoo.com
印度, Hyderabad, Telangana, 500007
G. Rajashekher Reddy
Natural Products Laboratory, Department of Chemistry
Email: prasadraoou@yahoo.com
印度, Hyderabad, Telangana, 500007
A. Sravani
Molecular Medicine and Therapeutics Laboratory, Centre for Plant Molecular Biology
Email: prasadraoou@yahoo.com
印度, Hyderabad, Telangana, 500007
K. Ramakrishna
Molecular Medicine and Therapeutics Laboratory, Centre for Plant Molecular Biology
Email: prasadraoou@yahoo.com
印度, Hyderabad, Telangana, 500007
Ch. Prasad Rao
Natural Products Laboratory, Department of Chemistry
编辑信件的主要联系方式.
Email: prasadraoou@yahoo.com
印度, Hyderabad, Telangana, 500007