Skip to content
2000
  1. Home
  2. A-Z Publications
  3. Current Chinese Chemistry
  4. Volume 1, Issue 1
  5. Article
Volume 1, Issue 1
  • ISSN: 2666-0016
  • E-ISSN: 2666-0008

Abstract

The treatment of cancer requires scientific advancement. ATP-competitive mTOR inhibitors have been studied as potential antitumor agents.

A series of substituted benzimidazole compounds were designed, synthesized and characterized via introducing 2-chloroquinolin into 2nd position and most title compounds exhibited enhanced anticancer activities.

To study the anticancer mechanism, was successfully docked by iGEMDOCK 2.0 which gives good affinity towards m-TOR/PI3K dual inhibitors. The anti-proliferative activities of these compounds were evaluated on MCF-7 and A549 cell line for Breast and lung cancer, respectively.

2-(2-chloroquinolin-3-yl)-1H-benzoimidazol-1-yl)(phenyl)methanone exhibited significant anti-proliferative activity, especially against breast cancer for MCF7 cell line and (2-(2-chloroquinolin-3-yl)-1H-benzo[d]imidazol-1-yl)(4-nitrophenyl)methanone was significantly active against lung cancer (IC50 89 µM) for A579 cell line.

gives more activity on breast cancer and it gives IC50 197 µM for MCF7 cell line and (2-(2-chloroquinolin-3-yl)-1H-benzo[d]imidazol-1-yl) (4-nitrophenyl) methanone lung cancer IC50 89 µM for A579 cell line.

© 2021 Bentham Science Publishers
Loading

Article metrics loading...

/content/journals/ccchem/10.2174/2666001601666200121163605
2021-03-01
2024-11-22

  • From This Site

    /content/journals/ccchem/10.2174/2666001601666200121163605
    dcterms_title,dcterms_subject,pub_keyword
    -contentType:Contributor -contentType:Concept -contentType:Institution
    10
    5
Loading full text...

Full text loading...

References

  1. PanchalI.I. BadeliyaS.N. PatelR. PatelA. DevaligarA. In silico analysis and molecular docking studies of novel 4-amino-3- (isoquinolin-4-yl)-1H-pyrazolo[3,4-d] pyrimidine derivatives as dual PI3-K/mTOR inhibitors.Curr. Drug Discov. Technol.201916329730610.2174/156800961866618110214493430387396
     [Google Scholar]
  2. MaoB. GaoS. WengY. ZhangL. ZhangL. Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors.Eur. J. Med. Chem.201712913515010.1016/j.ejmech.2017.02.01528235701
     [Google Scholar]
  3. MiaoZ. Yufang, Deng.; Lifeng, Z.; Guoyi, Y.; Fangying, Wang.; Ye Tian; Lanxi, Z.; Hongxia, J.; Yuanwei, C. Design, synthesis, and biological evaluation of dimorpholine substituted thienopyrimidines as potential class I PI3K/mTOR dual inhibitors.J. Med. Chem.2017604023403510.1021/acs.jmedchem.7b00357
     [Google Scholar]
  4. IshanI.P. RoshaniR. AshishD.P. Design, synthesis and pharmacological evalution of 1,3,4-Oxadiazole derivatives as collapsin response mediator protein 1 (CRMP 1) inhibitors.Curr. Drug Discov. Technol.201916111
     [Google Scholar]
  5. LeeJ.J. LohK. YapY.S. PI3K/Akt/mTOR inhibitors in breast cancer.Cancer Biol. Med.201512434235426779371
     [Google Scholar]
  6. Wise-DraperT.M. MoorthyG. SalkeniM.A. KarimN.A. ThomasH.E. MercerC.A. BegM.S. O’GaraS. OlowokureO. FathallahH. KozmaS.C. ThomasG. RixeO. DesaiP. MorrisJ.C.A.S. NaglaA.K. HalaE.T. CarolA.M. M, Shalaan. A phase Ib study of the dual PI3K/mTOR inhibitor Dactolisib (BEZ235) combined with everolimus in patients with advanced solid malignancies.Target. Oncol.201712332333210.1007/s11523‑017‑0482‑928357727
     [Google Scholar]
  7. FeiS. JinyingZ. HongyuL. LiangliangWu. HongyuJ. QiyanWu. The dual PI3K/mTOR inhibitor dactolisib elicits antitumor activity in vitro and in vivo.Oncotarget20182, 91706717
     [Google Scholar]
  8. MooreK.N. BauerT.M. FalchookG.S. ChowdhuryS. PatelC. NeuwirthR. EnkeA. ZohrenF. PatelM.R. Phase I study of the investigational oral mTORC1/2 inhibitor sapanisertib (TAK-228): tolerability and food effects of a milled formulation in patients with advanced solid tumours.ESMO Open201832e00029110.1136/esmoopen‑2017‑00029129464110
     [Google Scholar]
  9. JiangS.J. WangS. Dual targeting of mTORC1 and mTORC2 by INK-128 potently inhibits human prostate cancer cell growth in vitro and in vivo.Tumour Biol.201536108177818410.1007/s13277‑015‑3536‑625990456
     [Google Scholar]
  10. YangH. RudgeD.G. KoosJ.D. VaidialingamB. YangH.J. PavletichN.P. mTOR kinase structure, mechanism and regulation.Nature2013497744821722310.1038/nature1212223636326
     [Google Scholar]
  11. IshanP. AshishS. AnimeshD. UmangS. AshishP. AlkeshP. DhruboJ.S. In silico analysis and molecular docking studies of novel 6,7-dihydropyrano [2,3-d] pyrimidin-5-one derivatives as human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR) Inhibitors.Curr. Cancer Ther. Rev.201915113
     [Google Scholar]
  12. TekaleA.S. ShaikhS.A.L. Synthesis and characterisation of substituted quinoline by Vilsmeier-Haack reagent.Int. J. Chem. Stu.2017510104
     [Google Scholar]
/content/journals/ccchem/10.2174/2666001601666200121163605
Loading
Molecular Modelling, Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives for the Treatment of Breast Cancer
Curr Chin Chem 1, 11 (2021); https://doi.org/10.2174/2666001601666200121163605
/content/journals/ccchem/10.2174/2666001601666200121163605
/content/journals/ccchem/10.2174/2666001601666200121163605
Loading

Data & Media loading...


  • Article Type:     Research Article
Keyword(s): 2-chloroquinolin; anticancer; Benzimidazole derivatives; biological evaluation breast cancer; MCF7 cell line; molecular modelling

Most Cited Most Cited RSS feed

This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error
Please enter a valid_number test