SYNTHESIS AND MOLECULAR MODELING OF SIX NOVEL MONASTROL ANALOGUES: EVALUATION OF CYTOTOXICITY AND KINESIN INHIBITORY ACTIVITY AGAINST HELA CELL LINE

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ABNOUS KHALIL; BARATI BATOUL; MEHRI SOGHRA; MASBOGHI FARIMANI MOHAMMAD REZA; ALIBOLANDI MONA; MOHAMMADPOUR FATEMEH; GHANDADI MORTEZA; HADIZADEH FARZIN

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Journal: DARU Journal of Pharmaceutical Sciences Year:2013 | Volume:21 | Issue:9 Page(s): 1-8

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Title

SYNTHESIS AND MOLECULAR MODELING OF SIX NOVEL MONASTROL ANALOGUES: EVALUATION OF CYTOTOXICITY AND KINESIN INHIBITORY ACTIVITY AGAINST HELA CELL LINE

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Keywords

BIGINELLI REACTION

DIHYDROPYRIMIDINE

MITOTIC KINESIN EG5

DIMETHYLENASTRON

Abstract

Background and the purpose of the study: A common approach in cancer chemotherapy is development of drugs that interrupt the mitosis phase of cell division. DIMETHYLENASTRON is a known kinesin inhibitor. In this study, six novel DIMETHYLENASTRON analogues (4a-f), in which 3-hydroxyphenyl substituent has been replaced with substituted benzylimidazolyl, were synthesized through BIGINELLI REACTION.Methods: Six novel Biginelli compounds (4a-f) were synthesized through one step BIGINELLI REACTION of imidazole aldehydes (3a-c), dimedone and urea or thioura. In vitro cytotoxicities of prepared compounds were investigated using MTT assay. Furthermore the ELIPA kit was implemented to study inhibitory effects of synthesized compounds on ATPase activity of kinesin by measuring of organic phosphate.Results: Our results indicated that analogue 4c is the most toxic and analogues 4f, 4b and dimethylenasteron were less cytotoxic in compare with other analogues. On the other hand, analogue 4a, 4b, 4c and 4e showed stronger Kinesin inhibition as compared with analogue 4f and dimethylenasteron. None of synthesized compounds were as potent kinesin inhibitor as Taxol. Docking analysis revealed that hydrogen bond formation and hydrophobic interactions were the key factors affecting inhibitory effects of these compounds.Conclusion: Newly synthesized compounds were found to have moderate to good cytotoxicity against HeLa cancer cell. Our results may be helpful in further design of DIHYDROPYRIMIDINE as potential anticancer agents.

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APA: Copy

ABNOUS, KHALIL, BARATI, BATOUL, MEHRI, SOGHRA, MASBOGHI FARIMANI, MOHAMMAD REZA, ALIBOLANDI, MONA, MOHAMMADPOUR, FATEMEH, GHANDADI, MORTEZA, & HADIZADEH, FARZIN. (2013). SYNTHESIS AND MOLECULAR MODELING OF SIX NOVEL MONASTROL ANALOGUES: EVALUATION OF CYTOTOXICITY AND KINESIN INHIBITORY ACTIVITY AGAINST HELA CELL LINE. DARU JOURNAL OF PHARMACEUTICAL SCIENCE, 21(9), 1-8. SID. https://sid.ir/paper/275743/en

Vancouver: Copy

ABNOUS KHALIL, BARATI BATOUL, MEHRI SOGHRA, MASBOGHI FARIMANI MOHAMMAD REZA, ALIBOLANDI MONA, MOHAMMADPOUR FATEMEH, GHANDADI MORTEZA, HADIZADEH FARZIN. SYNTHESIS AND MOLECULAR MODELING OF SIX NOVEL MONASTROL ANALOGUES: EVALUATION OF CYTOTOXICITY AND KINESIN INHIBITORY ACTIVITY AGAINST HELA CELL LINE. DARU JOURNAL OF PHARMACEUTICAL SCIENCE[Internet]. 2013;21(9):1-8. Available from: https://sid.ir/paper/275743/en

IEEE: Copy

KHALIL ABNOUS, BATOUL BARATI, SOGHRA MEHRI, MOHAMMAD REZA MASBOGHI FARIMANI, MONA ALIBOLANDI, FATEMEH MOHAMMADPOUR, MORTEZA GHANDADI, and FARZIN HADIZADEH, “SYNTHESIS AND MOLECULAR MODELING OF SIX NOVEL MONASTROL ANALOGUES: EVALUATION OF CYTOTOXICITY AND KINESIN INHIBITORY ACTIVITY AGAINST HELA CELL LINE,” DARU JOURNAL OF PHARMACEUTICAL SCIENCE, vol. 21, no. 9, pp. 1–8, 2013, [Online]. Available: https://sid.ir/paper/275743/en

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