Abstract
Quinazoline scaffold has been successfully utilized for development of various inhibitors of tubulin, epidermal growth factor receptor (EGFR), polo like kinases (PLKs), Hedgehog-Gli signaling pathway and protein kinase B (PKB) /Akt pathway. Compounds based on quinazolines have shown efficacies in µM to nM range in various cancer cell lines and thus could be useful scaffolds for development of both apoptosis inducers as well as inhibitors. This compilation is based on various patents published till 2015 and divides the quinazolines in two main categories: Quinazolines as apoptosis inducers and as apoptosis inhibitors. These two main categories are further sub-categorized based on the use/pharmacological indications for these classes of patented compounds. This review will act as a tool for the researchers working on exploring the anticancer potential of quinazoline as a privileged heterocyclic. The promising anticancer profile of some of the quinazoline based compounds clearly highlights the clinical potential of this heterocycle.
Keywords: Apoptosis inducers, apoptosis inhibitors, cancer, caspases, p53, tubulin, quinazolines.
Recent Patents on Anti-Cancer Drug Discovery
Title:Quinazolines as Apoptosis Inducers and Inhibitors: A Review of Patent Literature
Volume: 11 Issue: 1
Author(s): Samir Mehndiratta, Sameer Sapra, Gurpreet singh, Manwinder Singh and Kunal Nepali
Affiliation:
Keywords: Apoptosis inducers, apoptosis inhibitors, cancer, caspases, p53, tubulin, quinazolines.
Abstract: Quinazoline scaffold has been successfully utilized for development of various inhibitors of tubulin, epidermal growth factor receptor (EGFR), polo like kinases (PLKs), Hedgehog-Gli signaling pathway and protein kinase B (PKB) /Akt pathway. Compounds based on quinazolines have shown efficacies in µM to nM range in various cancer cell lines and thus could be useful scaffolds for development of both apoptosis inducers as well as inhibitors. This compilation is based on various patents published till 2015 and divides the quinazolines in two main categories: Quinazolines as apoptosis inducers and as apoptosis inhibitors. These two main categories are further sub-categorized based on the use/pharmacological indications for these classes of patented compounds. This review will act as a tool for the researchers working on exploring the anticancer potential of quinazoline as a privileged heterocyclic. The promising anticancer profile of some of the quinazoline based compounds clearly highlights the clinical potential of this heterocycle.
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Mehndiratta Samir, Sapra Sameer, singh Gurpreet, Singh Manwinder and Nepali Kunal, Quinazolines as Apoptosis Inducers and Inhibitors: A Review of Patent Literature, Recent Patents on Anti-Cancer Drug Discovery 2016; 11 (1) . https://dx.doi.org/10.2174/1574892811666151218151506
DOI https://dx.doi.org/10.2174/1574892811666151218151506 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
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