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

In search of unprecedented tri and/or tetrapod pharmacophoric conjugates, a series of 32 new 4-ethyl-1H-benzo[b][1,4]diazepin-2(3H)-ones were synthesized and properly elucidated using MS, IR, NMR, and elemental analysis. In vitro investigation of 11 compounds of this series, using a panel of two hum...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Molecules (Basel, Switzerland) Switzerland), 2020-04, Vol.25 (9), p.2051, Article 2051
Hauptverfasser:	El Azab, Islam H., Elkanzi, Nadia A. A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenocarcinoma Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology benzodiazepine Benzodiazepines - chemical synthesis Benzodiazepines - pharmacology Biochemistry & Molecular Biology Breast Cell Line, Tumor Chemistry Chemistry Techniques, Synthetic Chemistry, Multidisciplinary Chemistry, Pharmaceutical - methods Colorectal carcinoma cyclocondensation reaction cytotoxic activity Cytotoxicity Doxorubicin Doxorubicin - pharmacology Drug Design Drug Screening Assays, Antitumor HCT116 Cells Humans Infrared analysis Inhibitory Concentration 50 Life Sciences & Biomedicine Magnetic Resonance Spectroscopy Mass Spectrometry MCF-7 Cells Molecular Structure N-heterocycles Physical Sciences Science & Technology Spectrophotometry, Infrared Tumor cell lines
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	In search of unprecedented tri and/or tetrapod pharmacophoric conjugates, a series of 32 new 4-ethyl-1H-benzo[b][1,4]diazepin-2(3H)-ones were synthesized and properly elucidated using MS, IR, NMR, and elemental analysis. In vitro 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 9 displayed maximum cytotoxicity with IC50 values of 16.19 +/- 1.35 and 17.16 +/- 1.54 mu M against HCT-116 and MCF-7, respectively, compared to standard drug doxorubicin.
ISSN:	1420-3049 1420-3049
DOI:	10.3390/molecules25092051