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Hydroxamates of para-aminobenzoic acid as selective inhibitors of HDAC8.
Kulandaivelu, Umasankar; Chilakamari, Laxmi Manasa; Jadav, Surender Singh; Rao, Tadikonda Rama; Jayaveera, K N; Shireesha, Boyapati; Hauser, Alexander-Thomas; Senger, Johanna; Marek, Martin; Romier, Christophe; Jung, Manfred; Jayaprakash, Venkatesan.
Afiliación
  • Kulandaivelu U; Medicinal Chemistry Research Division, Vaagdevi College of Pharmacy, Hanamkonda, Warangal 506 001, Andhra Pradesh, India.
  • Chilakamari LM; Medicinal Chemistry Research Division, Vaagdevi College of Pharmacy, Hanamkonda, Warangal 506 001, Andhra Pradesh, India.
  • Jadav SS; Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi 835 215, Jharkhand, India.
  • Rao TR; Blue Birds College Of Pharmacy, Hanamkonda, Warangal 506 015, Andhra Pradesh, India.
  • Jayaveera KN; Department of Chemistry, Jawaharlal Nehru Technological University Anantapur, College of Engineering, Anantapur 515 002, Andhra Pradesh, India.
  • Shireesha B; Medicinal Chemistry Research Division, Vaagdevi College of Pharmacy, Hanamkonda, Warangal 506 001, Andhra Pradesh, India.
  • Hauser AT; Institute of Pharmaceutical Sciences, Universität Freiburg, Albertstr. 25, 79104 Freiburg, Germany.
  • Senger J; Institute of Pharmaceutical Sciences, Universität Freiburg, Albertstr. 25, 79104 Freiburg, Germany.
  • Marek M; Integrated Structural Biology Department, IGBMC, 1 rue Laurent Fries, 67404 Illkirch, France.
  • Romier C; Integrated Structural Biology Department, IGBMC, 1 rue Laurent Fries, 67404 Illkirch, France.
  • Jung M; Institute of Pharmaceutical Sciences, Universität Freiburg, Albertstr. 25, 79104 Freiburg, Germany. Electronic address: manfred.jung@pharmazie.uni-freiburg.de.
  • Jayaprakash V; Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi 835 215, Jharkhand, India; Valens Pharma Services, Regus Citi Centre, Level 6, Chennai Citi Centre, 10/11, Dr. Radhakrishnan Salai, Chennai 600 004, Tamil Nadu, India. Electronic address: drvenkatesanj
Bioorg Chem ; 57: 116-120, 2014 Dec.
Article en En | MEDLINE | ID: mdl-25462986
ABSTRACT
A series of hydroxamates (4a-4l) were prepared from p-aminobenzoic acid to inhibit HDAC8. The idea is to substitute rigid aromatic ring in place of less rigid piperazine ring of hydroxamates reported earlier by our group. It is expected to increase potency retaining the selectivity. Result obtained suggested that the modifications carried out retained the selectivity towards HDAC8 isoform and increasing the potency in very few cases. Increase in potency is also associated with variation in cap aryl region. Two compounds (4f &4l) were found to inhibit HDAC8 at concentrations (IC50) less than 20µM.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Proteínas Represoras / Ácido 4-Aminobenzoico / Inhibidores de Histona Desacetilasas / Ácidos Hidroxámicos Tipo de estudio: Prognostic_studies Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2014 Tipo del documento: Article País de afiliación: India
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Proteínas Represoras / Ácido 4-Aminobenzoico / Inhibidores de Histona Desacetilasas / Ácidos Hidroxámicos Tipo de estudio: Prognostic_studies Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2014 Tipo del documento: Article País de afiliación: India