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Synthesis and antitumour evaluation of Monastrol and analogues - Synthesis of DHPMs via the Biginelli reaction and evaluation of their antitumour activity in U937 leukaemia cells. DE

English · Paperback / Softback

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Cancer is a disease with a high incidence and mortality rate and is responsible for around 12 per cent of all deaths worldwide. For this reason, there is great interest in developing compounds with cytotoxic activity, especially with the aim of getting round the problem of resistance. The aim of this book was to synthesise six dihydropyrimidinones (DHPMs) and investigate their antitumour activity against a leukaemic cell line (U937). The compounds have hydroxyl groups in the ortho, meta and para positions of the benzene ring and oxygen or sulphur in the pyrimidine ring. After synthesising the compounds under thermal conditions and microwave irradiation, the DHPMs were evaluated for antitumour activity using the MTT metabolisation method. The sulphur portion in the structures of the DHPMs significantly increased the antitumour activity for the U937 leukaemia cell type. This was confirmed by the reduction in IC50 to 84 mimol.L-1. This study found that the position of the hydroxyl group in the benzene ring influences the antitumour activity observed for U937 leukaemia cells, showing that the hydroxyl group in the ortho position of the benzene ring is the most active.

About the author










She has a degree and a bachelor's degree in chemistry, a master's degree in organic chemistry from UFRRJ, a PhD in organic chemistry from USP and a post-doctorate in catalysis from UFRJ. She has experience in organic synthesis and catalysis involving microwave irradiation. She is currently Professor of Organic Chemistry at UFRJ.

Product details

Authors Victor Hugo C. Milla, Wagner Silva Terra, Andréa L. Ferreira de Souza
Publisher Our Knowledge Publishing
 
Languages English
Product format Paperback / Softback
Released 26.08.2023
 
EAN 9786206386230
ISBN 9786206386230
No. of pages 52
Subject Natural sciences, medicine, IT, technology > Chemistry > Organic chemistry

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