Synthesis and ribonucleotide reductase inhibitory activity of thiosemicarbazones

K Krishnan, K Prathiba, V Jayaprakash, A Basu…

Index: Krishnan, Kesavan; Prathiba, Kumari; Jayaprakash, Venkatesan; Basu, Arijit; Mishra, Nibha; Zhou, Bingsen; Hu, Shuya; Yen, Yun Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 23 p. 6248 - 6250

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Citation Number: 26

Abstract

Ribonucleotide reductase (RR) is an important therapeutic target for anticancer drugs. The structure of human RR features a 1: 1 complex of two homodimeric subunits, hRRM1 and hRRM2. Prokaryotically expressed and highly purified recombinant human RR subunits, hRRM1 and hRRM2, were used for holoenzyme-based [3H] CDP reduction in vitro assay. Ten new thiosemicarbazones (7–16) were synthesized and screened for their RR ...