Literature DB >> 18976907

Synthesis and ribonucleotide reductase inhibitory activity of thiosemicarbazones.

Kesavan Krishnan1, Kumari Prathiba, Venkatesan Jayaprakash, Arijit Basu, Nibha Mishra, Bingsen Zhou, Shuya Hu, Yun Yen.   

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 [(3)H]CDP reduction in vitro assay. Ten new thiosemicarbazones (7-16) were synthesized and screened for their RR inhibitory activity. Two thiosemicarbazones derived from p-hydroxy benzaldehyde (9 and 10) were found to be active but less potent than the standard, Hydroxyurea (HU). Guided by the activity of compounds 9 and 10, 11 new thiosemicarbazones (17-27) derived from p-hydroxy benzaldehyde were prepared and screened for their RR inhibitory activity. All the 11 compounds were more potent than HU.

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Year:  2008        PMID： 18976907     DOI： 10.1016/j.bmcl.2008.09.097

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Understanding the molecular interactions of different radical scavengers with ribonucleotide reductase M2 (hRRM2) domain: opening the gates and gaining access.

Authors:  Arijit Basu; Barij N Sinha
Journal:  J Comput Aided Mol Des       Date:  2012-05-26       Impact factor: 3.686

2.  In vitro and in vivo cytotoxic activity and human serum albumin interaction for a methoxy-styryl-thiosemicarbazone.

Authors:  Otávio Augusto Chaves; Isabela S de Castro; Carla Marins Goulart; Myrtes S S Bellieny; José Carlos Netto-Ferreira; Juliana Echevarria-Lima; Aurea Echevarria
Journal:  Invest New Drugs       Date:  2019-01-19       Impact factor: 3.850

3.  Synthesis, DNA Binding, and Antiproliferative Activity of Novel Acridine-Thiosemicarbazone Derivatives.

Authors:  Sinara Mônica Vitalino de Almeida; Elizabeth Almeida Lafayette; Lúcia Patrícia Bezerra Gomes da Silva; Cézar Augusto da Cruz Amorim; Tiago Bento de Oliveira; Ana Lucia Tasca Gois Ruiz; João Ernesto de Carvalho; Ricardo Olímpio de Moura; Eduardo Isidoro Carneiro Beltrão; Maria do Carmo Alves de Lima; Luiz Bezerra de Carvalho Júnior
Journal:  Int J Mol Sci       Date:  2015-06-09       Impact factor: 5.923

4.  Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives.

Authors:  Nazar Trotsko; Agata Przekora; Justyna Zalewska; Grażyna Ginalska; Agata Paneth; Monika Wujec
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

5.  Novel platinum(II) and palladium(II) complexes of thiosemicarbazones derived from 5-substitutedthiophene-2-carboxaldehydes and their antiviral and cytotoxic activities.

Authors:  Ayşegül Karaküçük-İyidoğan; Demet Taşdemir; Emine Elçin Oruç-Emre; Jan Balzarini
Journal:  Eur J Med Chem       Date:  2011-10-01       Impact factor: 6.514

Review 6.  Role of pH in Regulating Cancer Pyrimidine Synthesis.

Authors:  Saad Saeed Alqahtani; Tomas Koltai; Muntaser E Ibrahim; Adil H H Bashir; Sari T S Alhoufie; Samrein B M Ahmed; Daria Di Molfetta; Tiago M A Carvalho; Rosa Angela Cardone; Stephan Joel Reshkin; Abdelhameed Hifny; Mohamed E Ahmed; Khalid Omer Alfarouk
Journal:  J Xenobiot       Date:  2022-07-06
  6 in total

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