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Open AccessArticle

New Potent 5α- Reductase and Aromatase Inhibitors Derived from 1,2,3-Triazole Derivative

1
Chemistry Department, Faculty of Sciences, University of Sharjah, Sharjah 27272, UAE
2
Chemistry of Natural and Microbial Products Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, Cairo 12622, Egypt
3
Research and Development Unit, Saco Pharm. Co., 6 October City 11632, Egypt
*
Author to whom correspondence should be addressed.
Molecules 2020, 25(3), 672; https://doi.org/10.3390/molecules25030672
Received: 21 January 2020 / Revised: 3 February 2020 / Accepted: 3 February 2020 / Published: 5 February 2020
(This article belongs to the Section Bioorganic Chemistry)
This work describes the utility of pyrazole-4-carbaldehyde 1 as starting material for the synthesis of a novel potent series of 5α-reductase and aromatase inhibitors derived from 1,2,3-triazole derivative. Condensation of 1 with active methylene and different amino pyrazoles produced the respective Schiff bases 24, 8 and 9. On the other hand, 1 was reacted with ethyl cyanoacetate and thiourea in one-pot reaction to afford the pyrazolo-6- thioxopyridin-2-[3H]-one (10). Moreover, α–β unsaturated chalcone derivative 11 was prepared via the reaction of compound 1 with P-methoxy acetophenone, which in turn reacted with each of ethyl cyanoacetate, malononitrile, hydrazine hydrate, and thiosemicarbazide to afford the corresponding pyridine and pyrazole derivatives 13, 14, 17, and 20. The structure of newly synthesized compounds was characterized by analytical and spectroscopic data (IR, MS and NMR). All new compounds were evaluated against 5α-reductase and aromatase inhibitors and the results showed that many of these compounds inhibit 5α-reductase and aromatase activity; compound 13 was found to be the highest potency among the tested samples comparing with the reference drugs. View Full-Text
Keywords: 1,2,3-triazoles; 5-α reductase inhibitors; aromatase inhibitors; hormone-dependent cancer 1,2,3-triazoles; 5-α reductase inhibitors; aromatase inhibitors; hormone-dependent cancer
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MDPI and ACS Style

El-Naggar, M.; Abd El-All, A.S.; El-Naem, S.I.A.; Abdalla, M.M.; Rashdan, H.R.M. New Potent 5α- Reductase and Aromatase Inhibitors Derived from 1,2,3-Triazole Derivative. Molecules 2020, 25, 672. https://doi.org/10.3390/molecules25030672

AMA Style

El-Naggar M, Abd El-All AS, El-Naem SIA, Abdalla MM, Rashdan HRM. New Potent 5α- Reductase and Aromatase Inhibitors Derived from 1,2,3-Triazole Derivative. Molecules. 2020; 25(3):672. https://doi.org/10.3390/molecules25030672

Chicago/Turabian Style

El-Naggar, Mohamed; Abd El-All, Amira S.; El-Naem, Shweekar I.A.; Abdalla, Mohamed M.; Rashdan, Huda R.M. 2020. "New Potent 5α- Reductase and Aromatase Inhibitors Derived from 1,2,3-Triazole Derivative" Molecules 25, no. 3: 672. https://doi.org/10.3390/molecules25030672

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