An Efficient Synthetic Approach Towards Benzo[]pyrano[2,3-][1,4]diazepines, and Their Cytotoxic Activity.

Molecules

On leave from Chemistry Department, Faculty of Science, Aswan University, Aswan, P.O. Box, Aswan 81528, Egypt.

Published: April 2020


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Article Abstract

In search of unprecedented tri and/or tetrapod pharmacophoric conjugates, a series of 32 new 4-ethyl-1-benzo[][1,4]diazepin-2(3)-ones were synthesized and properly elucidated using MS, IR, NMR, and elemental analysis. investigation of 11 compounds of this series, using a panel of two human tumor cell lines namely; human breast adenocarcinoma (MCF-7), and human colorectal carcinoma (HCT-116), revealed promising cytotoxic activities. Among all synthesized compounds, analogue displayed maximum cytotoxicity with IC values of 16.19 ± 1.35 and 17.16 ± 1.54 μM against HCT-116 and MCF-7, respectively, compared to standard drug doxorubicin.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7248725PMC
http://dx.doi.org/10.3390/molecules25092051DOI Listing

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