Curcumin inspired 2-chloro/phenoxy quinoline analogues: Synthesis and biological evaluation as potential anticancer agents
| Autor: | Lalita Guntuku, V.G.M. Naidu, P.V. Sri Ramya, Ahmed Kamal, Chander Singh Digwal, Srinivas Angapelly, Shailaja Karri, Bathini Nagendra Babu |
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| Rok vydání: | 2018 |
| Předmět: |
Curcumin
Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Apoptosis 01 natural sciences Biochemistry Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Annexin Cell Line Tumor Drug Discovery Humans Structure–activity relationship DAPI Cytotoxicity Molecular Biology Cell Proliferation Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Cell growth Organic Chemistry Quinoline Cell Cycle Checkpoints In vitro 0104 chemical sciences chemistry 030220 oncology & carcinogenesis Quinolines Molecular Medicine Drug Screening Assays Antitumor |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 28:892-898 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2018.01.070 |
| Popis: | Synthesis of twenty new curcumin inspired 2-chloro/phenoxy quinoline derivatives is outlined in this study. The obtained new chemical entities were screened in vitro for their cytotoxic activity towards various tumor cell lines. Of the compounds screened, 6c and 9d exhibited significant activity and the most active analogue 6c displayed promising cytotoxicity against PC-3 (IC50 of 3.12 ± 0.11 μM), DU-145, NCI-H460 and 4 T1 cell lines. Further, 6c and 9d have 2.1 and 1.4 times more aqueous solubility, respectively, than curcumin. Additionally, the promising candidate 6c could induce G2/M cell cycle arrest and apoptosis in PC-3 cells, as determined by AO-EB staining, DAPI staining, analysis of ROS levels as well as annexin binding assay. |
| Databáze: | OpenAIRE |
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