Identification of novel quinazolinone hybrids as cytotoxic agents against C6 glioma cell lines

Novel quinazolinone‐triazole hybrid heterocycles were identified as cytotoxic agents to inhibit glioblastoma cell proliferation. These compounds were synthesized using click reaction by building a triazole linker on quinazolinone and tested for cytotoxicity on C6 glioma cell lines, a facsimile of gl...

Full description

Saved in:
Bibliographic Details
Published in:Journal of the Chinese Chemical Society (Taipei) 2022-06, Vol.69 (6), p.968-978
Main Authors: Pagilla, Shankaraiah, Anagani Kanaka Durga, Bhavani, Vodnala, Sumathi, Kamutam, Ramakrishna, Mudiraj, Anwita, Phanithi, Prakash Babu, Chetti, Prabhakar
Format: Article
Language:English
Subjects:
anticancer activity
C6 glioma cell lines
Chemical reactions
Chemical synthesis
click reaction
Molecular docking
Quinazolinones
quinazolin‐4(3H)‐one
rat thymidylate synthase
Toxicity testing
triazole
Triazoles
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Novel quinazolinone‐triazole hybrid heterocycles were identified as cytotoxic agents to inhibit glioblastoma cell proliferation. These compounds were synthesized using click reaction by building a triazole linker on quinazolinone and tested for cytotoxicity on C6 glioma cell lines, a facsimile of glioblastoma multiforme. Few of these series significantly reduced the proliferation of cell lines with IC50 8–15 μM and may act as fetching leads for glioblastoma therapies. The binding affinity and ligand‐receptor interaction between hybrids and rat thymidylate synthase were investigated using molecular docking techniques. A new series of quinazolin‐4(3H)‐ones tethered with 1,2,3‐triazolyl moiety as drug leads or drug intermediates against glioblastoma were developed. The target hybrid molecules were designed to attain better activity and selectivity towards cancer cells by introducing the lipophilic methoxybenzene moiety as a linker between quinazolin‐4 (3H)‐one and 1,2,3‐triazole scaffolds.
ISSN:0009-4536
2192-6549
DOI:10.1002/jccs.202200058