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  3. Curcumin inspired 2-chloro/phenoxy quinoline analogues: Synthesis and biological evaluation as potential anticancer agents

Curcumin inspired 2-chloro/phenoxy quinoline analogues: Synthesis and biological evaluation as potential anticancer agents

  • Bioorg Med Chem Lett. 2018 Mar 1;28(5):892-898. doi: 10.1016/j.bmcl.2018.01.070.
P V Sri Ramya 1,  Lalita Guntuku 2,  Srinivas Angapelly 1,  Shailaja Karri 2,  Chander Singh Digwal 1,  Bathini Nagendra Babu 1,  V G M Naidu 2,  Ahmed Kamal 3
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
  • 2 Department of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
  • 3 Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India; School of Pharmaceutical Education and Research (SPER), Jamia Hamdard University, New Delhi 110062, India. Electronic address: ahmedkamal@iict.res.in.
PMID: 29429834 DOI: 10.1016/j.bmcl.2018.01.070
Abstract

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.

Keywords

2-Substituted quinolines; Anticancer; Apoptosis; Claisen-Schmidt condensation; Curcumin mimics.

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