Synthesis, X-Ray Crystal Structures, and Preliminary Antiproliferative Activities of New s-Triazine-hydroxybenzylidene Hydrazone Derivatives
Joint Authors
Barakat, Assem
Al-Majid, A. M. A.
Al-Rasheed, Hessa H.
Almarhoon, Zainab M.
El-Senduny, Fardous F.
Ghabbour, Hazem A.
El-Faham, Ayman
Badria, Farid A.
Source
Issue
Vol. 2019, Issue 2019 (31 Dec. 2019), pp.1-10, 10 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2019-04-30
Country of Publication
Egypt
No. of Pages
10
Main Subjects
Abstract EN
We herein report a new small library of Schiff-base compounds that encompasses s-triazine and (2 or 4)-hydroxylbenzylidene derivatives.
These compounds were synthesized through a hydrazone linkage connecting both the s-triazine and hydroxybenzylidene derivatives.
The synthetic strategy adopted allowed the synthesis of the target compounds with excellent yields and purities as observed from their NMR (1H and 13C) and elemental analysis.
Furthermore, 4f, 5b, and 5f were further confirmed by X-ray single crystal diffraction technique.
The preliminary antiproliferative activities for the synthesized compounds were tested against two different cancer cell lines including breast cancer (MCF-7) and colon cancer (HCT-116).
From the eighteen compounds, which have been examined, only two derivatives having piperidine moiety showed more selectivity against the two cell lines MCF-7 and HCT-116, while the others showed very weak activity.
The position of the hydroxyl group in the benzylidine ring and the substituent on the s-triazine moiety has great effect on the activity of the prepared compounds.
The IC50 values for the two derivatives 4a and 5a evaluated against breast cancer cells, very close to those for the chemotherapeutic drug cisplatin, are 27 µM (13.3 µg/mL), 17 µM (8.4 µg/mL), and 20 µM (6 µg/mL) for 4a, 5a, and cisplatin, respectively.
These results propose the preliminary antiproliferative activity of these two derivatives may deserve further consideration for development of new derivatives as potent anticancer agents.
American Psychological Association (APA)
Barakat, Assem& El-Senduny, Fardous F.& Almarhoon, Zainab M.& Al-Rasheed, Hessa H.& Badria, Farid A.& Al-Majid, A. M. A.…[et al.]. 2019. Synthesis, X-Ray Crystal Structures, and Preliminary Antiproliferative Activities of New s-Triazine-hydroxybenzylidene Hydrazone Derivatives. Journal of Chemistry،Vol. 2019, no. 2019, pp.1-10.
https://search.emarefa.net/detail/BIM-1172045
Modern Language Association (MLA)
Barakat, Assem…[et al.]. Synthesis, X-Ray Crystal Structures, and Preliminary Antiproliferative Activities of New s-Triazine-hydroxybenzylidene Hydrazone Derivatives. Journal of Chemistry No. 2019 (2019), pp.1-10.
https://search.emarefa.net/detail/BIM-1172045
American Medical Association (AMA)
Barakat, Assem& El-Senduny, Fardous F.& Almarhoon, Zainab M.& Al-Rasheed, Hessa H.& Badria, Farid A.& Al-Majid, A. M. A.…[et al.]. Synthesis, X-Ray Crystal Structures, and Preliminary Antiproliferative Activities of New s-Triazine-hydroxybenzylidene Hydrazone Derivatives. Journal of Chemistry. 2019. Vol. 2019, no. 2019, pp.1-10.
https://search.emarefa.net/detail/BIM-1172045
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1172045