Open AccessArticle
Design, Synthesis, and In Vitro Antiproliferative Screening of New Hydrazone Derivatives Containing cis-(4-Chlorostyryl) Amide Moiety
by
Tarfah Al-Warhi, Leena S. Alqahtani, Matokah Abualnaja, Saba Beigh, Ola A. Abu Ali, Fahmy G. Elsaid, Ali A. Shati, Rasha Mohammed Saleem, Ali Hassan Ahmed Maghrabi, Amani Abdulrahman Alharthi, Amal Alyamani, Eman Fayad, Ali H. Abu Almaaty, Islam Zaki and Shaimaa Hamouda
Cited by 6 | Viewed by 1843
Abstract
Hydrazones are regarded as a distinctive category of organic compounds because of their tremendous characteristics and potential uses in analytical, chemical, and medicinal chemistry. In the present study, a new series of Hydrazone Derivatives bearing
cis-(4-chlorostyryl) amide moiety were designed and synthesized.
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Hydrazones are regarded as a distinctive category of organic compounds because of their tremendous characteristics and potential uses in analytical, chemical, and medicinal chemistry. In the present study, a new series of Hydrazone Derivatives bearing
cis-(4-chlorostyryl) amide moiety were designed and synthesized. In vitro cytotoxicity screening showed that compounds
3i,
3l,
3m, and
3n revealed potent anticancer activity against MCF-7 cancer cell line with IC
50 values between 2.19–4.37 μM compared with Staurosporin as a reference compound. The antiproliferative activity of these compounds appears to be correlated well with their ability to inhibit the VEGFR-2 kinase enzyme. Activation of the damage response pathway leads to cellular cycle arrest at the G1 phase. Fluorochrome Annexin V/PI staining indicated that cell death proceeds through the apoptotic pathway mechanism. The mechanistic pathway was confirmed by a significant increase in the level of active
caspase 9 compared with control untreated MCF-7 cells.
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