2. Academic Validation
  3. Quinoline-azetidinone hybrids: Synthesis and in vitro antiproliferation activity against Hep G2 and Hep 3B human cell lines

Quinoline-azetidinone hybrids: Synthesis and in vitro antiproliferation activity against Hep G2 and Hep 3B human cell lines

  • Bioorg Med Chem Lett. 2017 Apr 1;27(7):1566-1571. doi: 10.1016/j.bmcl.2017.02.043.
S G Alegaon 1,  P Parchure 2,  L D Araujo 2,  P S Salve 2,  K R Alagawadi 2,  S S Jalalpure 3,  V M Kumbar 4
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Chemistry, KLE University's College of Pharmacy, Nehru Nagar, Belagavi 590010, Karnataka, India. Electronic address: sgalegaon@klepharm.edu.
  • 2 Department of Pharmaceutical Chemistry, KLE University's College of Pharmacy, Nehru Nagar, Belagavi 590010, Karnataka, India.
  • 3 Department of Pharmacognosy, KLE University's College of Pharmacy, Nehru Nagar, Belagavi 590010, Karnataka, India; Dr. Prabhakar Kore Basic Science Research Center, KLE University, Nehru Nagar, Belagavi 590010, Karnataka, India.
  • 4 Dr. Prabhakar Kore Basic Science Research Center, KLE University, Nehru Nagar, Belagavi 590010, Karnataka, India.
PMID: 28262527 DOI: 10.1016/j.bmcl.2017.02.043
Abstract

In search of new heterocyclic Anticancer agents, a new quinoline-azetidinone hybrid template have been designed, synthesized and screened for their cytotoxic activity against human Cancer cell lines such as Hep G2, and Hep 3B by the MTT assay and results were compared with paclitaxel, 5-fluorouracil and doxorubicin. Interestingly, some of the compounds were found significantly active against both cell lines. The compound 6f (IC50=0.04±0.01µM) exhibited potent antiproliferation activity against Hep G2 cell line, and 6j compound (IC50=0.66±0.01µM) demonstrated potent antiproliferation activity against Hep 3B cell line and provide to be more potent as cytotoxic agents than standard drugs. Morphological changes suggest the induction of Apoptosis and describe the mechanism of action of these hybrid antitumor agents.

Keywords

Antiproliferation; Azetidinone; Drug likeness; Quinoline.

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