SYNTHESIS OF TWO NOVEL DERIVATIVES OF CYCLOSPORIN A AND EVALUATION OF THEIR ANTIPROLIFERATIVE EFFECT ON CANCER CELL LINES
Abdelazem, A., Lee, S. (2022). SYNTHESIS OF TWO NOVEL DERIVATIVES OF CYCLOSPORIN A AND EVALUATION OF THEIR ANTIPROLIFERATIVE EFFECT ON CANCER CELL LINES. EKB Journal Management System, 45(1), 191-199. doi: 10.21608/bfsa.2022.239431
Ahmed Z. Abdelazem; So Ha Lee. "SYNTHESIS OF TWO NOVEL DERIVATIVES OF CYCLOSPORIN A AND EVALUATION OF THEIR ANTIPROLIFERATIVE EFFECT ON CANCER CELL LINES". EKB Journal Management System, 45, 1, 2022, 191-199. doi: 10.21608/bfsa.2022.239431
Abdelazem, A., Lee, S. (2022). 'SYNTHESIS OF TWO NOVEL DERIVATIVES OF CYCLOSPORIN A AND EVALUATION OF THEIR ANTIPROLIFERATIVE EFFECT ON CANCER CELL LINES', EKB Journal Management System, 45(1), pp. 191-199. doi: 10.21608/bfsa.2022.239431
Abdelazem, A., Lee, S. SYNTHESIS OF TWO NOVEL DERIVATIVES OF CYCLOSPORIN A AND EVALUATION OF THEIR ANTIPROLIFERATIVE EFFECT ON CANCER CELL LINES. EKB Journal Management System, 2022; 45(1): 191-199. doi: 10.21608/bfsa.2022.239431

SYNTHESIS OF TWO NOVEL DERIVATIVES OF CYCLOSPORIN A AND EVALUATION OF THEIR ANTIPROLIFERATIVE EFFECT ON CANCER CELL LINES

Bulletin of Pharmaceutical Sciences Assiut University
Article 16, Volume 45, Issue 1, June 2022, Page 191-199  XML PDF (878.57 K)
Document Type: Original Article
DOI: 10.21608/bfsa.2022.239431
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Authors
Ahmed Z. Abdelazem email orcid 1; So Ha Lee2
1Biotechnology & Life Sciences Department, Faculty of Postgraduate Studies for Advanced Sciences, Beni-Suef University, Beni-Suef 62517, Egypt
2Chemical Kinomics Research Center, Korea Institute of Science and Technology, Hwarangno 14-gil 5, Seongbuk-gu, Seoul 136-791, Republic of Korea
Abstract
Two novel derivatives of cyclosporin A were designed and synthesized. Synthesis of target compounds has been performed using olefin metathesis chemistry. The structures of target compounds were confirmed using 1H and 13C NMR and high-resolution mass spectroscopy. The in vitro antiproliferative effect of the two compounds was tested over NCI-60 cancer cell lines of nine different cancer types. The piperidinedione derivative (compound 7) had an inhibitory effect higher than 80% over 13 cancer cell lines, and close to or higher than 100% over six cancer cell lines. Compound 7 showed also significantly higher inhibitory activity than cyclosporin A against non-small cell lung cancer NCI-H226 cell line. Moreover, compound 7 showed an overall moderate antiproliferative activity against the NCI-60 cancer cell lines with a mean value of 57.54 %. While, the pyrrolidindione derivative (compound 6) showed weak antiproliferative activity against the NCI-60 cancer cell lines with a mean value of 28.83%. Finally, the predicted pharmacokinetic properties of compounds 6 and 7 were better than that of cyclosporine A.
Keywords
Synthesis; Anti-proliferative effect; Cyclosporin A; olefin metathesis; pharmacokinetic
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