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Synthesis of Novel Steroidal 17α-Triazolyl Derivatives Via Cu(I)-Catalyzed Azide-Alkyne Cycloaddition and their Evaluation as Potential Progestational Agents

Magda M F Ismail1, Dalia H Soliman1, Nehad M A Eldydamony2, G A Abdel Jaleel3, and Adel F Youssef2, 4
1 Department of Pharmaceutical chemistry, Faculty of Pharmacy (Girls), Al-Azhar University.
2 Department of Medicinal Chemistry, College of Pharmacy and Pharmaceutical Industry, MUST.
3 Department of Pharmacology, National Research Center.
4 Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University.
Abstract—Many progestins have been developed for use in contraception, Hormone Replacement Therapy (HRT), menopausal hormone therapy and treatment of gynecological diseases. Progestins are also highly efficacious in decreasing the occurrence of endometrial hyperplasia and carcinoma caused by unopposed estrogens. Click reaction was adapted for the condensation of the terminal ethynyl group of norethindroneenanthate (NET-EN)3 and levonorgestrel (LNG)5 with substituted phenyl azides2a-c to prepare 1, 4-disubstituted-1, 2, 3-triazole derivatives 4a-c and 6a-c. The assigned structures were confirmed by spectroscopic and element microanalytical data. Biological screening of the prepared compounds was undertaken to evaluate possible progestational activity on rat uterus in vivo and ex vivo on the isolated rat uterus. The histopathologic changes of the uterus associated with the new compounds and the reference drugs NET-EN and LNG encompass a variety of morphologic features that were interpreted. All the prepared compounds conserve their progestational activity, significantly much higher than vehicle. Compound 4c showed activity parameters higher than NET-EN, while 6b matched those displayed by LNG. Compound 4b displayed 200 fold the uterolytic effect of NET-EN. On the other hand, LNG derivatives showed uterolytic effect much weaker than the parent drug. Molecular modeling studies were performed using MOE software (V.10.2010) to further corroborate the biological assay results acquired for this new group of compounds and gain insight into their plausible mode of interaction(s) within the progesterone receptor.

Index Terms—Click reaction, Steroidal azoles, Progestational activity, Uterolytic effect, Molecular modeling, Copper catalyzed azide-alkyne cycloaddition

Cite: Magda M F Ismail, Dalia H Soliman, Nehad M A Eldydamony, G A Abdel Jaleel, and Adel F Youssef, "Synthesis of Novel Steroidal 17α-Triazolyl Derivatives Via Cu(I)-Catalyzed Azide-Alkyne Cycloaddition and their Evaluation as Potential Progestational Agents," International Journal of Pharma Medicine and Biological Sciences, Vol. 3, No. 3, pp. 58-79, July 2014.
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