Anti-prostate cancer and anti-EGFR activities of new Nilutamide-isoxazole hybrids

Nilutamide-isoxazole hybrids

Authors

  • Ashwini Nagaraju Chaitanya Deemed to be University
  • Satheesh Kumar Nukala Chaitanya Deemed to be University
  • Narasimha Swamy Thirukovela Chaitanya Deemed to be University
  • Ravinder Manchal Chaitanya Deemed to be University

Keywords:

Nilutamide, Isoxazole, Prostate cancer, EGFR inhibition , Drug derivates, click chemistry

Abstract

Herein, synthesis of new Nilutamide-isoxazoles (5a-5n) via Cu(I)-promoted one-pot reaction between 1-(but-3-yn-1-yl)-5,5-dimethyl-3-(4-nitro-3-(trifluoromethyl)phenyl)imidazolidine-2,4-dione (3) and several aldehydes (4a-4n) in benign aq. tbutanol as key approach has been reported. The in vitro growth inhibition activity of all these compounds revealed that the majority of compounds were more active against DU-145 in comparison to PC3. Particularly, compounds 5f, 5h and 5k showed greater activity against DU-145 than the standard drug 5-Fluoro Uracil with IC50 values <30 mM. whereas compound 5g showed comparable activity against DU-145 cell line with the positive control. The Epidermal growth factor receptor (EGFR) is well known to be expressed in DU-145 cancer cells, the most potent compounds 5f, 5h and 5k were then screened for their inhibitory potential against tyrosine kinase EGFR and found that compounds 5f and 5k showed remarkable inhibition with MIVs 93.4% and 91.3% respectively, while compound 5h displayed good inhibition (MIV = 84.6%) as compared to the Erlotinib.

URN:NBN:sciencein.cbl.2023.v10.542

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Author Biographies

  • Ashwini Nagaraju, Chaitanya Deemed to be University

    Department of Chemistry

  • Satheesh Kumar Nukala, Chaitanya Deemed to be University

    Department of Chemistry

  • Narasimha Swamy Thirukovela, Chaitanya Deemed to be University

    Department of Chemistry

  • Ravinder Manchal, Chaitanya Deemed to be University

    Department of Chemistry

Published

2023-03-20

Issue

Section

Short Communications

URN

How to Cite

(1)
Nagaraju, A.; Nukala, S. K.; Thirukovela, N. S.; Manchal, R. Anti-Prostate Cancer and Anti-EGFR Activities of New Nilutamide-Isoxazole Hybrids. Chem Biol Lett 2023, 10 (3), 542.

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