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

Raju Bathula,Shobha Rani Satla,Presenjit Mondal,Ramakrishna Raparla

doi:10.1186/s43094-020-00059-5

Abstract

BackgroundA 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.MethodsThe 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.ResultsThe 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.ConclusionBased on the experimental evidences, we proposed structure activity relationship to provide significant information for the design and development of further potent anticancer agents.

Highlights

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
The cancer cell lines used for the study were human breast cancer cell line (MCF-7) and human lung adenocarcinoma (A-549), were sub-cultured in-house, in PGP life Sciences, Hyderabad, India
The results of the cytotoxic activity of the tested compounds using MTT assay confirmed that the compounds 7d, 7f, 7g, and 7h exhibited satisfactory cytotoxic activity in A-549 lung adenocarcinoma cancer cells

Summary

Introduction

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. Quinazoline and quinazolinone mixes are likewise utilized in planning of different useful materials for engineered science and present in different medication particles. Pyrroles and their derivatives were found most important classes of heterocyclic compounds. They prove extensive pharmacological properties such as anti-inflammatory [14], antioxidant [15], antitumor [16], antifungal [17], antibacterial [18], and immune suppressant activities [19]. This survey is an endeavor to extend the immense probability and concentrated on the different natural exercises of quinazolines and quinazolinones [20]. The anticancer activity of previously reported few quinazoline-based [24, 25] and pyrrole-based [26]

Methods

Results

Discussion

Conclusion