Bio Chem Press  Internet Electronic Journal of Molecular Design is a refereed journal for scientific papers regarding all applications of molecular design
Home | News | Current Issue | Journal Index | IECMD 2004 | Preprint Index | Instructions for Authors | Send the Manuscript | Special Issue
 BioChemPress.com  To bookmark this site press Ctrl D
 
   Home
   News & Announcements
  Journal Info
   Current Issue
   Journal Index
   Preprint Index
   Editor
   Advisory Board
  Conference Info
   IECMD 2004
   Day 1
   Day 2
   Day 3
   Day 4
   Day 5
   Day 6
   Day 7
   Day 8
   Day 9
   Day 10
   IECMD 2003
  BioChem Links
   CoEPrA
   Support Vector Machines
  Author Info
   Instructions for Authors
   Send the Manuscript
   Special Issue
  Contact
   Editorial Office
   Subscription
   Advertising
   Copyright
  User Info
   Terms of Use
   License

Internet Electronic Journal of Molecular Design - IEJMD, ISSN 1538-6414, CODEN IEJMAT
ABSTRACT - Internet Electron. J. Mol. Des. October 2002, Volume 1, Number 10, 488-502

1,5-N,N-Disubstituted-2-(Substituted Benzenesulphonyl)-Glutamamides as Antitumor Agents. Part 2. Synthesis, Biological Activity and QSAR Study
Bikash Debnath, Kolluru Srikanth, Suchandra Banarjee, and Tarun Jha
Internet Electron. J. Mol. Des. 2002, 1, 488-502

Free: Download the paper in PDF format Return to Table of Contents Get Acrobat Reader to view and print the paper

Abstract:
Cancer has been described as a nitrogen trap. Tumor cells are avid glutamine consumers. Glutamine (GLN), which is a glutamic acid derivative, supplies its amide nitrogen to tumor cells in the biosynthesis of purine and pyrimidine bases. Isoglutamines, which have 1-N-amide instead of 5-N-amide and 5-COOH instead of 1-COOH in glutamine, showed antitumor activities. Thus, compounds containing both 1- and 5-amido group (i.e. glutamamide) may have potential antitumor activity. In continuation of our complex program for the development of new potential anticancer agents through rational drug design, 28 new 1,5-N,N-disubstituted-2-(3,4-disubstituted benzenesulphonyl)-glutamamides were selected for synthesis, biological evaluation and QSAR study. These compounds were synthesized and screened against Ehrlich Ascites Carcinoma (EAC) cells in Swiss Albino mice. A QSAR study was performed in order to design leads with increased effectiveness for antitumor activity using the Hansch approach. Some of the synthesized compounds showed excellent yields and several of then were found to have good antitumor activity. The QSAR study showed that low hydrophobic or hydrophilic substitution at benzene ring, electron withdrawing group at para and electron donating group at meta position of benzene ring and less bulky alkyl substitution at aliphatic side chain may result in appreciable antitumor activity. This study throws some light in the future design of this type of compounds with better anticancer activity.

Free: Download the paper in PDF format Return to Table of Contents Get Acrobat Reader to view and print the paper

Home | News | Current Issue | Journal Index | IECMD 2004 | Preprint Index | Instructions for Authors | Send the Manuscript | Special Issue
Last changes: January 5, 2006 Webmaster
http://www.biochempress.com/
Copyright © 2001-2006 Ovidiu Ivanciuc