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Related Concept Videos

Cancer Therapies02:49

Cancer Therapies

Cancer therapies are various modes of treatment, such as surgery, radiation therapy, and chemotherapy that are administered to cancer patients.
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
Cancer Therapies02:49

Cancer Therapies

Cancer therapies are various modes of treatment, such as surgery, radiation therapy, and chemotherapy that are administered to cancer patients.
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Cancer Prevention02:59

Cancer Prevention

Several factors can increase the risk of cancer in an individual. About 50% of cancer cases can be prevented by adopting a healthy lifestyle, regular exercise, eating healthy, and following a modest cancer prevention diet. Epidemiological studies have consistently shown that populations with vegetable and fruit-rich diets have reduced the incidence of cancer. On the other hand, populations who have a diet rich in animal fat, red meat, junk food, or high calories are predisposed to cancer.
Some...
Electron Transport Chain: Complex I and II01:46

Electron Transport Chain: Complex I and II

The mitochondrial electron transport chain (ETC) is the main energy generation system in the eukaryotic cells. However, mitochondria also produce cytotoxic reactive oxygen species (ROS) due to the large electron flow during oxidative phosphorylation. While Complex I is one of the primary sources of superoxide radicals, ROS production by Complex II is uncommon and may only be observed in cancer cells with mutated complexes.
ROS generation is regulated and maintained at moderate levels necessary...

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Related Experiment Video

Updated: May 31, 2026

Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
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Published on: February 9, 2019

Licofelone-nitric oxide donors as anticancer agents.

Wukun Liu1, Jinpei Zhou, Yinglin Liu

  • 1College of Chemistry and Chemical Engineering, Hunan University, Changsha, P.R. China.

Archiv Der Pharmazie
|June 18, 2011
PubMed
Summary

New licofelone nitric oxide donor conjugates show potent anticancer activity against breast and colon cancer cells. These compounds demonstrate higher cytotoxicity than licofelone, potentially due to increased nitric oxide production.

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Published on: July 20, 2019

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Cancer Biology

Background:

  • Licofelone is a non-steroidal anti-inflammatory drug with known anticancer properties.
  • Nitric oxide (NO) donors are investigated for their therapeutic potential in cancer treatment.
  • Developing novel drug conjugates can enhance therapeutic efficacy and target specificity.

Purpose of the Study:

  • To synthesize and evaluate novel licofelone-nitric oxide donor conjugates for anticancer activity.
  • To assess the antiproliferative and cytotoxic effects of these conjugates on various cancer cell lines.
  • To investigate the relationship between nitric oxide production, COX inhibition, and cytotoxic activity.

Main Methods:

  • Parallel synthesis approach was utilized to create five licofelone nitric oxide donor conjugates.
  • Biological screening involved assessing antiproliferative potency against MCF-7, MDA-MB-231 (breast cancer), and HT-29 (colon cancer) cell lines.
  • Cytotoxicity and COX-1/COX-2 inhibitory activity were evaluated for the synthesized compounds.

Main Results:

  • Conjugates with propyl (6b), butyl (6c), and octyl (6d) chains exhibited significant antiproliferative activity.
  • Compounds 6b-d showed at least a 2-fold increase in cytotoxicity against MDA-MB-231 cells compared to licofelone.
  • The novel conjugates displayed reduced inhibitory activity against COX-1 and COX-2 compared to the parent compound.

Conclusions:

  • Licofelone nitric oxide donor conjugates, particularly those with propyl, butyl, or octyl linkers, are promising anticancer agents.
  • The enhanced cytotoxicity of these conjugates is likely attributed to elevated nitric oxide production rather than COX inhibition.
  • Further research into these NO-donating conjugates could lead to novel cancer therapeutics.