Literature DB >> 20605448

Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity.

Bhadaliya Chetan1, Mahesh Bunha, Monika Jagrat, Barij Nayan Sinha, Philipp Saiko, Geraldine Graser, Thomas Szekeres, Ganapathy Raman, Praveen Rajendran, Dhatchana Moorthy, Arijit Basu, Venkatesan Jayaprakash.   

Abstract

Six compounds were synthesized with piperazine in linker region and hydroxamate as Zinc Binding Group (ZBG). They were screened against three cancer cell-lines (NCIH460; HCT116; U251). Compounds 5c and 5f with GI(50) value of 9.33+/-1.3 microM and 12.03+/-4 microM, respectively, were tested for their inhibitory potential on hHDAC8. Compound 5c had IC(50) of 33.67 microM. Compounds were also screened for their anticancer activity against HL60 human promyelocytic leukemia cell line due to the presence of pharmacophoric features of RR inhibitors in them. Compound 5c had IC(50) of 0.6 microM at 48h. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20605448     DOI： 10.1016/j.bmcl.2010.05.020

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


  6 in total

1.  Chemical scaffolds with structural similarities to siderophores of nonribosomal peptide-polyketide origin as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis.

Authors:  Julian A Ferreras; Akash Gupta; Neal D Amin; Arijit Basu; Barij N Sinha; Stefan Worgall; Venkatesan Jayaprakash; Luis E N Quadri
Journal:  Bioorg Med Chem Lett       Date:  2011-08-26       Impact factor: 2.823

2.  Identification of 3-(piperazinylmethyl)benzofuran derivatives as novel type II CDK2 inhibitors: design, synthesis, biological evaluation, and in silico insights.

Authors:  Wagdy M Eldehna; Raed M Maklad; Hadia Almahli; Tarfah Al-Warhi; Eslam B Elkaeed; Mohammed A S Abourehab; Hatem A Abdel-Aziz; Ahmed M El Kerdawy
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

3.  Exploring the anti-cancer activity of novel thiosemicarbazones generated through the combination of retro-fragments: dissection of critical structure-activity relationships.

Authors:  Maciej Serda; Danuta S Kalinowski; Nathalie Rasko; Eliška Potůčková; Anna Mrozek-Wilczkiewicz; Robert Musiol; Jan G Małecki; Mieczysław Sajewicz; Alicja Ratuszna; Angelika Muchowicz; Jakub Gołąb; Tomáš Simůnek; Des R Richardson; Jaroslaw Polanski
Journal:  PLoS One       Date:  2014-10-16       Impact factor: 3.240

4.  Brønsted acid-mediated cyclization-dehydrosulfonylation/reduction sequences: An easy access to pyrazinoisoquinolines and pyridopyrazines.

Authors:  Ramana Sreenivasa Rao; Chinnasamy Ramaraj Ramanathan
Journal:  Beilstein J Org Chem       Date:  2017-03-07       Impact factor: 2.883

5.  Biological evaluation and structure activity relationship of 9-methyl-1-phenyl-9H-pyrido[3,4-b]indole derivatives as anti-leishmanial agents.

Authors:  Penta Ashok; Subhash Chander; Terry K Smith; Rajnish Prakash Singh; Prabhat Nath Jha; Murugesan Sankaranarayanan
Journal:  Bioorg Chem       Date:  2018-11-22       Impact factor: 5.275

6.  Regioselective addition of Grignard reagents to N-acylpyrazinium salts: synthesis of substituted 1,2-dihydropyrazines and Δ5-2-oxopiperazines.

Authors:  Valentine R St Hilaire; William E Hopkins; Yenteeo S Miller; Srinivasa R Dandepally; Alfred L Williams
Journal:  Beilstein J Org Chem       Date:  2019-01-08       Impact factor: 2.883
  6 in total

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