Synthesis and Characterization of New Dihydronaphthalene Candidates as Potent Cytotoxic Agents against MCF-7 Human Cancer Cells
المؤلفون المشاركون
Ahmed, Nesreen S.
Sarhan, Alaadin E.
Al-Ashmawy, Aisha A. K.
Amr, Abd El-Galil E.
Haiba, Mogedda E.
Elsayed, Elsayed A.
المصدر
العدد
المجلد 2020، العدد 2020 (31 ديسمبر/كانون الأول 2020)، ص ص. 1-10، 10ص.
الناشر
Hindawi Publishing Corporation
تاريخ النشر
2020-12-30
دولة النشر
مصر
عدد الصفحات
10
التخصصات الرئيسية
الملخص EN
In the present work, a new series of dihydronaphthalene derivatives were synthesized starting with 6-methoxy-1-tetralone 1, and the corresponding hydrazine derivative 2.
Reaction of compound 2 with aryl isothiocyanates produced thiosemicarbazides 3a-d, which were reacted with ethyl chloroacetate to give thiazolidinone derivatives 4a-d.
Pyrano thiazolecarbonitrile derivatives 5a-f were prepared by heating a mixture of compounds 4a or 4c, aryl aldehydes, and malononitrile utilizing distilled water in the presence of catalytic amount of potassium hydrogen phthalate.
Also, treatment of 4a with DMF-DMA under solvent-free conditions gave enaminone derivative 6, which condensed with ethyl acetoacetate or acetylacetone or malononitrile or cyanothioacetamide to give compounds 7-10, respectively.
Finally, reaction of the enaminone 6 with 2-aminoimidazol or 2-aminothiazol in the presence of glacial acetic acid produced derivatives 11 and 12, respectively.
Cytotoxic evaluation of eleven compounds, against MCF-7 (human breast adenocarcinoma) cell lines, was estimated.
Results revealed that five of the examined compounds 5a, 5d, 5e, 10, and 3d showed potent cytotoxic activities recording, IC50 values; 0.93±0.02, 1.76±0.04, 2.36±0.06, 2.83±0.07, and 3.73±0.09 μM, respectively, which were more potent than the reference used (Saturosporin, IC506.08±0.15 μM).
The new products were also examined towards normal epithelial breast cells (MCF10A).
All of them showed very good safety profile with different degrees and were safer than the reference drug used.
Compound 5a was the most effective against MCF-7 cells and was less toxic than Saturosporin by about 18.45-folds towards MCF01A normal cells.
All the new compounds were fully characterized by the different spectral and analytical tools.
Herein, detailed syntheses, spectroscopic, and biological data are reported.
نمط استشهاد جمعية علماء النفس الأمريكية (APA)
Ahmed, Nesreen S.& Sarhan, Alaadin E.& Al-Ashmawy, Aisha A. K.& Amr, Abd El-Galil E.& Haiba, Mogedda E.& Elsayed, Elsayed A.. 2020. Synthesis and Characterization of New Dihydronaphthalene Candidates as Potent Cytotoxic Agents against MCF-7 Human Cancer Cells. BioMed Research International،Vol. 2020, no. 2020, pp.1-10.
https://search.emarefa.net/detail/BIM-1137572
نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)
Ahmed, Nesreen S.…[et al.]. Synthesis and Characterization of New Dihydronaphthalene Candidates as Potent Cytotoxic Agents against MCF-7 Human Cancer Cells. BioMed Research International No. 2020 (2020), pp.1-10.
https://search.emarefa.net/detail/BIM-1137572
نمط استشهاد الجمعية الطبية الأمريكية (AMA)
Ahmed, Nesreen S.& Sarhan, Alaadin E.& Al-Ashmawy, Aisha A. K.& Amr, Abd El-Galil E.& Haiba, Mogedda E.& Elsayed, Elsayed A.. Synthesis and Characterization of New Dihydronaphthalene Candidates as Potent Cytotoxic Agents against MCF-7 Human Cancer Cells. BioMed Research International. 2020. Vol. 2020, no. 2020, pp.1-10.
https://search.emarefa.net/detail/BIM-1137572
نوع البيانات
مقالات
لغة النص
الإنجليزية
الملاحظات
Includes bibliographical references
رقم السجل
BIM-1137572
قاعدة معامل التأثير والاستشهادات المرجعية العربي "ارسيف Arcif"
أضخم قاعدة بيانات عربية للاستشهادات المرجعية للمجلات العلمية المحكمة الصادرة في العالم العربي
تقوم هذه الخدمة بالتحقق من التشابه أو الانتحال في الأبحاث والمقالات العلمية والأطروحات الجامعية والكتب والأبحاث باللغة العربية، وتحديد درجة التشابه أو أصالة الأعمال البحثية وحماية ملكيتها الفكرية. تعرف اكثر