Synthesis and cytotoxicity studies of Hedgehog enzyme inhibitors SANT-1 and GANT-61 as anticancer agents

Venugopal Chenna, Chaoxin Hu, Saeed R. Khan

Research output: Contribution to journalArticle

Abstract

Cancer-related death is one of the most common causes of mortality in society. Small molecules have the capability to disrupt aberrant signaling pathways in tumors, leading to anticancer activities. Therefore the search for new molecules for cancer treatment continues to draw attention to the scientific research community. Synthesis and biological evaluation of hedgehog (Hh) pathway inhibitors SANT-1 and GANT-61 are disclosed. These molecules have been synthesized from common precursors using simple conversions, our synthesis features Vils-Meier-Haack reaction, imine formation reaction and N-arylation reaction. These drugs were evaluated using a Hh reporter assay to confirm pathway inhibitory activity, and tested for cell viability against pancreatic and prostate cancer cells. These methodologies can be applied to make potent analogs of both inhibitors.

Original languageEnglish (US)
Pages (from-to)641-647
Number of pages7
JournalJournal of Environmental Science and Health - Part A Toxic/Hazardous Substances and Environmental Engineering
Volume49
Issue number6
DOIs
StatePublished - May 12 2014

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Enzyme Inhibitors
Cytotoxicity
Antineoplastic Agents
Enzymes
Molecules
Cells
Neoplasms
Imines
Oncology
Pancreatic Neoplasms
Tumors
Assays
Prostatic Neoplasms
Cell Survival
Mortality
Research
Pharmaceutical Preparations
GANT 61

Keywords

  • GANT-61
  • Hedgehog pathway
  • imine formation
  • N-arylation
  • SANT-1
  • Wills-Meyer-Hack reaction

ASJC Scopus subject areas

  • Environmental Engineering
  • Medicine(all)

Cite this

Synthesis and cytotoxicity studies of Hedgehog enzyme inhibitors SANT-1 and GANT-61 as anticancer agents. / Chenna, Venugopal; Hu, Chaoxin; Khan, Saeed R.

In: Journal of Environmental Science and Health - Part A Toxic/Hazardous Substances and Environmental Engineering, Vol. 49, No. 6, 12.05.2014, p. 641-647.

Research output: Contribution to journalArticle

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