Synthesis and biological evaluation of 1,3,4-oxadiazole linked azaindole derivatives as anticancer agents

A new library of 1,3,4-oxadiazole linked azaindole derivatives (11a-j) and their structures confirmed by spectroscopic techniques. Further, compounds were investigated for their anticancer applications towards four human cancer cell lines like PC3, DU-145 (prostate cancer), A549 (lung cancer) and MC...

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Bibliographic Details
Published in:Chemical Data Collections 2023-04, Vol.44, p.100981, Article 100981
Main Authors: Kumar, B.V.V. Satish, Douglas, S. Paul, Sandhya, Jonnala, Krishnakanth Reddy, L., Kiran, Gangarapu
Format: Article
Language:English
Subjects:
1,3,4-Oxadiazole
Azaindol
Indole
Rucaparib
Zibotentan
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Summary:A new library of 1,3,4-oxadiazole linked azaindole derivatives (11a-j) and their structures confirmed by spectroscopic techniques. Further, compounds were investigated for their anticancer applications towards four human cancer cell lines like PC3, DU-145 (prostate cancer), A549 (lung cancer) and MCF-7 (breast cancer) using MTT assay and etoposide use as positive control. Most of the synthesized compounds showed good to moderate activities. Among them, these compounds 11a, 11e, 11f, 11g and 11h displayed most promising anticancer activity on four cell lines. Especially, one compound 11f (PC3=0.011±0.0019µM; A549= 0.071±0.0028µM; MCF-7=0.023±0.0024µM; and DU-145= 0.16±0.077µM) showed more potent activity. The synthesized compounds were also performed molecular docking studies against the EGFR target (PDB ID: 1M17).
ISSN:2405-8300
2405-8300
DOI:10.1016/j.cdc.2022.100981