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Updated: Jun 9, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis of bioactive polyheterocyclic ring systems as 5α-reductase inhibitors
Naglaa A Abdel Hafez1, Thoraya A Farghaly, Mohamed A Al-Omar
1Department of Applied Organic Chemistry, National Research Center, Dokki, Cairo, Egypt.
Abstract:
Simple synthetic strategies for the hitherto unreported [1,2,4]triazolo[4,3-a]pyrido[4,3-d]pyrimidines 8 and [1,2,4]triazolo[4',3':1,2]pyrimido[4,5-b][1,6]naphthyridine-5-one 15 are described based on reaction of thione 3 and 12 with hydrazonoyl chloride 1a-h, respectively. The structures of products 8 and 15 were confirmed by spectroscopic and X-ray crystallographic analyses. Also, the mechanism of such reactions was discussed. In addition, reaction of compound 12 with bromoacetic acid and hydrazine hydrate was investigated. Compounds were screened against 5α-reductase and showed activities with good LD(50) and LD(90) for all compounds.
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