Literature DB >> 28262527

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

S G Alegaon1, P Parchure2, L D Araujo2, P S Salve2, K R Alagawadi2, S S Jalalpure3, V M Kumbar4.   

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.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antiproliferation; Azetidinone; Drug likeness; Quinoline

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Year:  2017        PMID: 28262527     DOI: 10.1016/j.bmcl.2017.02.043

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Tailored Quinolines Demonstrate Flexibility to Exert Antitumor Effects through Varied Mechanisms-A Medicinal Perspective.

Authors:  Sachin Sharma; Arshdeep Singh; Sahil Sharma; Ram Sharma; Jagjeet Singh; Nihar Kinarivala; Kunal Nepali; Jing P Liou
Journal:  Anticancer Agents Med Chem       Date:  2021       Impact factor: 2.527

2.  Molecular-docking-guided design, palladium-catalyzed synthesis and anticancer activity of paclitaxel-benzoxazoles hybrids.

Authors:  Ting Jiang; Ya-Nan Cao; Jin-Bu Xu; Feng Gao; Ling-Li Zheng
Journal:  Sci Rep       Date:  2022-06-15       Impact factor: 4.996

  2 in total

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