Literature DB >> 17383883

3-(3,4,5-Trimethoxyphenyl)-1-oxo-2-propene: a novel pharmacophore displaying potent multidrug resistance reversal and selective cytotoxicity.

Umashankar Das1, Masami Kawase, Hiroshi Sakagami, Atsushi Ideo, Jun Shimada, Joseph Molnár, Zoltán Baráth, Zsuzsanna Bata, Jonathan R Dimmock.   

Abstract

This study revealed that various alicyclic and acyclic compounds containing the 3-(3,4,5-trimethoxyphenyl)-2-propenoyl group displayed potent MDR reversal properties. In particular, a concentration of 4 microg/ml of 2,5-bis(3,4,5-trimethoxyphenylmethylene)cyclopentanone was 31 times more potent than verapamil as a MDR revertant. In general, they were selectively toxic to malignant rather than normal cells. Two representative compounds induced apoptosis in human HL-60 cells and markedly activated caspase-3.

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Year:  2007        PMID： 17383883     DOI： 10.1016/j.bmc.2007.03.022

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  10 in total

1.  A general HPLC-UV method for the quantitative determination of curcumin analogues containing the 1,5-diaryl-3-oxo-1,4-pentadienyl pharmacophore in rat biomatrices.

Authors:  Ravi Shankar Prasad Singh; Umashankar Das; Jonathan R Dimmock; Jane Alcorn
Journal:  J Chromatogr B Analyt Technol Biomed Life Sci       Date:  2010-09-20       Impact factor: 3.205

2.  Cytotoxic 2-benzylidene-6-(nitrobenzylidene)cyclohexanones which display substantially greater toxicity for neoplasms than non-malignant cells.

Authors:  Umashankar Das; Alireza Doroudi; H Inci Gul; Hari N Pati; Masami Kawase; Hiroshi Sakagami; Qing Chu; James P Stables; Jonathan R Dimmock
Journal:  Bioorg Med Chem       Date:  2010-02-04       Impact factor: 3.641

3.  1,3-diaryl-2-propenones and 2-benzylidene-1,3-indandiones: a quest for compounds displaying greater toxicity to neoplasms than normal cells.

Authors:  Hari N Pati; Umashankar Das; Hiroshi Sakagami; Masame Kawase; Qing Chu; Qintao Wang; James P Stables; Jonathan R Dimmock
Journal:  Arch Pharm (Weinheim)       Date:  2010-09       Impact factor: 3.751

4.  E,E-2-Benzylidene-6-(nitrobenzylidene)cyclohexanones: syntheses, cytotoxicity and an examination of some of their electronic, steric, and hydrophobic properties.

Authors:  Umashankar Das; Alireza Doroudi; Swagatika Das; Brian Bandy; Jan Balzarini; Erik De Clercq; Jonathan R Dimmock
Journal:  Bioorg Med Chem       Date:  2008-04-16       Impact factor: 3.641

5.  (2E,5E)-2,5-Bis(3,4,5-trimethoxy-benzyl-idene)cyclo-penta-none.

Authors:  Yi-Feng Sun; Yang Liu; Feng-Yu Zhang; Hong-Ji Chen; Yi-Ping Cui
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-09-20

6.  2-(3-Aryl-2-propenoyl)-3-methylquinoxaline-1,4-dioxides: a novel cluster of tumor-specific cytotoxins which reverse multidrug resistance.

Authors:  Umashankar Das; Hari N Pati; Atulya K Panda; Erik De Clercq; Jan Balzarini; Joseph Molnár; Zoltán Baráth; Imre Ocsovszki; Masami Kawase; Li Zhou; Hiroshi Sakagami; Jonathan R Dimmock
Journal:  Bioorg Med Chem       Date:  2009-04-17       Impact factor: 3.641

7.  1-[4-(2-Aminoethoxy)phenylcarbonyl]-3,5-bis-(benzylidene)-4-oxopiperidines: a novel series of highly potent revertants of P-glycoprotein associated multidrug resistance.

Authors:  Umashankar Das; Joseph Molnár; Zoltán Baráth; Zsuzsanna Bata; Jonathan R Dimmock
Journal:  Bioorg Med Chem Lett       Date:  2008-05-16       Impact factor: 2.823

8.  The cytotoxic properties and preferential toxicity to tumour cells displayed by some 2,4-bis(benzylidene)-8-methyl-8-azabicyclo[3.2.1] octan-3-ones and 3,5-bis(benzylidene)-1-methyl-4-piperidones.

Authors:  Hari N Pati; Umashankar Das; Swagatika Das; Brian Bandy; Erik De Clercq; Jan Balzarini; Masami Kawase; Hiroshi Sakagami; J Wilson Quail; James P Stables; Jonathan R Dimmock
Journal:  Eur J Med Chem       Date:  2008-03-29       Impact factor: 6.514

9.  1-Aryl-2-dimethylaminomethyl-2-propen-1-one hydrochlorides and related adducts: A quest for selective cytotoxicity for malignant cells.

Authors:  Hari N Pati; Umashankar Das; Masami Kawase; Hiroshi Sakagami; Jan Balzarini; Erik De Clercq; Jonathan R Dimmock
Journal:  Bioorg Med Chem       Date:  2008-03-27       Impact factor: 3.641

10.  A facile solvent free Claisen-Schmidt reaction: synthesis of α,α'-bis-(substituted-benzylidene)cycloalkanones and α,α'-bis-(substituted-alkylidene)cycloalkanones.

Authors:  A F M Motiur Rahman; Roushown Ali; Yurngdong Jahng; Adnan A Kadi
Journal:  Molecules       Date:  2012-01-09       Impact factor: 4.411
  10 in total

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