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

Future Journal of Pharmaceutical Sciences

Raju Bathula¹  Shobha Rani Satla¹  Ramakrishna Raparla²  Presenjit Mondal² 

[1] Centre for Pharmaceutical Science, Jawaharlal Nehru Technological University;Department of Pharmaceutical Chemistry, Vaageswari Institute of Pharmaceutical Sciences;

关键词: Quinazolines;    Pyrrole;    Cytotoxic;    Breast cancer;    Adenocarcinoma;   

DOI  :  10.1186/s43094-020-00059-5

来源: DOAJ

【 摘 要 】

Abstract 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, 1HNMR, 13C 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 (IC50 value 41.05 μM at 72 h). The synthesized compounds 7d and 7f were found effective in breast cancer cell line with IC50 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 IC50 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.

【 授权许可】

Unknown