Abstract
In an attempt to discover a potent and selective anticancer agent, gallic acid has been modified to benzylidene indanones as tubulin polymerization inhibitors. These compounds were evaluated against several human cancer cell lines and also evaluated for inhibition of tubulin polymerase in in vitro assays. Three of the analogues exhibited strong cytotoxicity against human cancer cell lines IC 50 = 10-880 nM and also showed tubulin polymerization inhibition (IC 50 = 0.62-2.04 μM). Compound 9j, the best candidate of the series was found to be non-toxic in acute oral toxicity in Swiss-albino mice up to 1000 mg/kg dose.
| Original language | English |
|---|---|
| Pages (from-to) | 3049-3057 |
| Number of pages | 9 |
| Journal | Bioorganic & Medicinal Chemistry |
| Volume | 20 |
| Issue number | 9 |
| DOIs | |
| Publication status | Published - 1 May 2012 |
| Externally published | Yes |
Bibliographical note
Funding Information:The authors are very much thankful to the Director, CSIR–CIMAP for constant encouragement and support. The CSIR Diamond Jubilee Research Internship to one of the authors (APP) is duly acknowledged. This research was supported by Council of Scientific and Industrial Research (CSIR), India. The most of the work is covered in Indian patent (No. 133NF2011) and US patent Provisional application no. 2769DEL2011, dt. 22-09-2011.
Funding
The authors are very much thankful to the Director, CSIR–CIMAP for constant encouragement and support. The CSIR Diamond Jubilee Research Internship to one of the authors (APP) is duly acknowledged. This research was supported by Council of Scientific and Industrial Research (CSIR), India. The most of the work is covered in Indian patent (No. 133NF2011) and US patent Provisional application no. 2769DEL2011, dt. 22-09-2011.
Keywords
- Acute oral toxicity
- Anticancer
- Gallic acid
- Indanones
- Tubulin polymerization inhibition
