Skip to main content
padlock icon - secure page this page is secure

Biological Evaluation of Indole Appended Triazolothiadiazepine Conjugates as Potent Anticancer Agents

Buy Article:

$68.00 + tax (Refund Policy)

Background: Cancer is one of the major health and socio-economic problems of the world even though extensive progress has been made in terms of early diagnosis and cure. The research for new anticancer drug development with more effective treatment is a field of utmost importance in current drug discovery.

Method: Molecular Hybridization (MH) strategy has been adapted for the rational design of new ligands, where pharmacophoric sub-unities in the molecular structure of two bioactives will lead to the design of new hybrid architectures. All the synthesized compounds (3a-z) were evaluated in HeLa and MCF-7 cell lines for their anticancer activity and compared against H9C2 normal cells.

Results: As expected, among the tested compounds, 3a, 3d, 3g, 3j, 3m and 3s exhibited highest activity with GI50 value of 1.72 μm, 2.10 μm, 4.26 μm, 2.43 μm, 5.11 μm and 4.34μm in HeLa cells and 1.86 μm, 2.50 μm, 5.20 μm, 4.40 μm, 6.14 μm and 5.30 μm in MCF-7 cells respectively. We also found that the compounds were non-toxic to H9C2 cells up to 20 μM.

Conclusion: Preliminary structure-activity relationship studies revealed that compounds with para-Cl substituted phenyl and 5-Cl substituted indole on diazepine ring proved to be more potent.
No References
No Citations
No Supplementary Data
No Article Media
No Metrics

Keywords: HeLa & MCF-7; Indole analogues; SAR studies; chalcones; cytotoxic activity; molecular hybridization; triazolothiadiazepines

Document Type: Research Article

Publication date: December 1, 2018

More about this publication?
  • The journal aims to provide updates to researchers about new bioactive compounds with proven activities in various biological screenings and pharmacological models. The journal will contain information about the structures, biological activities and sources of chemical entities discovered or designed by researchers and published in leading journals. The aim is to provide a valuable information source of bioactive compounds synthesized or isolated, which can be used for further development of pharmaceuticals by industry and academia.

    The journal should prove to be essential reading for pharmacologists, pharmaceutical chemists and medicinal chemists who wish to be kept informed and up-to-date with the latest and most important developments about new bioactive compounds of natural or synthetic origin, including recent patents.
  • Editorial Board
  • Information for Authors
  • Subscribe to this Title
  • Ingenta Connect is not responsible for the content or availability of external websites
  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more