Evaluation of antitumor potential of synthesized novel 2-substituted 4-anilinoquinazolines as quinazoline-pyrrole hybrids in MCF-7 human breast cancer cell line and A-549 human lung adenocarcinoma cell lines
Background A series of novel 2 substituted 4-anilinoquinazolines-pyrrole hybrids were synthesized, and cytotoxic activity were evaluated using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay. Methods The cell line used for the activity was MCF-7 breast cancer cell line and...
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Published in | Future journal of pharmaceutical sciences Vol. 6; no. 1; pp. 44 - 11 |
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Main Authors | , , , |
Format | Journal Article |
Language | English |
Published |
Berlin/Heidelberg
Springer Berlin Heidelberg
31.07.2020
Springer Nature B.V SpringerOpen |
Subjects | |
Online Access | Get full text |
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Summary: | Background
A series of novel 2 substituted 4-anilinoquinazolines-pyrrole hybrids were synthesized, and cytotoxic activity were evaluated using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay.
Methods
The cell line used for the activity was MCF-7 breast cancer cell line and A459 human lung adenocarcinoma cell line. The newly quinazoline-pyrrole hybrid compounds have been synthesized from the 4-chloro-7-(3-chloropropoxy)-6-methoxy-2-phenylquinazoline derivatives. The chemical structure of the synthesized compounds has been confirmed by FTIR,
1
HNMR,
13
C NMR, and mass spectral data. The cytotoxic study was conducted using morphological study and MTT assay against adenocarcinoma and human breast cancer cell lines.
Results
The results of cytotoxic evaluation revealed that few compounds show moderate to promising activity when compared with standard doxorubicin (IC
50
value 41.05 μM at 72 h). The synthesized compounds 7d and 7f were found effective in breast cancer cell line with IC
50
values 40.64 μM and 44.98 μM at 72 h, respectively. The synthesized compounds 7d, 7f, 7g, and 7h were found effective in adenocarcinoma cell line with IC
50
values of 41.05 μM, 45.54 μM, 46.93 μM, and 48.62 μM, respectively.
Conclusion
Based on the experimental evidences, we proposed structure activity relationship to provide significant information for the design and development of further potent anticancer agents. |
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ISSN: | 2314-7253 2314-7245 2314-7253 |
DOI: | 10.1186/s43094-020-00059-5 |