Journal
JOURNAL OF MOLECULAR STRUCTURE
Volume 1200, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.molstruc.2019.127097
Keywords
4(3H)-quinazolinone; Cytotoxicity; MDA-MB-231; Cell migration; Colony formation
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Funding
- DoP, Ministry of Chemicals & Fertilizers, Govt. of India of NIPER fellowship
- Department of science and technology Govt. of India [EMR/2017/000220]
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A series of new 4(3H)-quinazolinones were synthesized and evaluated for their cytotoxic activity against a set of human cancer cell lines MDA-MB-231 and MCF-7 (breast), HCT-116 and HT-29 (colon) and A549 (lung). Among the tested compounds, 22a exhibited promising cytotoxic activity against MDA-MB-231 (IC50: 3.21 mu M) and HT-29 (IC50: 7.23 mu M) cell lines. The mechanism of action and the apoptosis inducing effect of the compound 22a were studied using the breast cancer cell line MDA-MB-231. Treatment of MDA-MB-231 cell line with compound 22a showed typical apoptotic morphology like cell shrinkage, chromatin condensation and horseshoe shaped nuclei formation. Flow cytometric analysis indicated that the compound induces G0/G1 phase of cell cycle arrest in a dose dependent manner. The binding modes of the potent compounds with EGFR target protein were investigated by docking studies. (C) 2019 Elsevier B.V. All rights reserved.
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