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 language | English (US) |
|---|---|
| Pages (from-to) | 641-647 |
| Number of pages | 7 |
| Journal | Journal of Environmental Science and Health - Part A Toxic/Hazardous Substances and Environmental Engineering |
| Volume | 49 |
| Issue number | 6 |
| DOIs | |
| State | Published - May 12 2014 |
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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 journal › Article
}
TY - JOUR
T1 - Synthesis and cytotoxicity studies of Hedgehog enzyme inhibitors SANT-1 and GANT-61 as anticancer agents
AU - Chenna, Venugopal
AU - Hu, Chaoxin
AU - Khan, Saeed R.
PY - 2014/5/12
Y1 - 2014/5/12
N2 - 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.
AB - 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.
KW - GANT-61
KW - Hedgehog pathway
KW - imine formation
KW - N-arylation
KW - SANT-1
KW - Wills-Meyer-Hack reaction
UR - http://www.scopus.com/inward/record.url?scp=84896703564&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84896703564&partnerID=8YFLogxK
U2 - 10.1080/10934529.2014.865425
DO - 10.1080/10934529.2014.865425
M3 - Article
C2 - 24521409
AN - SCOPUS:84896703564
VL - 49
SP - 641
EP - 647
JO - Journal of Environmental Science and Health - Part A Toxic/Hazardous Substances and Environmental Engineering
JF - Journal of Environmental Science and Health - Part A Toxic/Hazardous Substances and Environmental Engineering
SN - 1093-4529
IS - 6
ER -