Quinazoline derivatives as potential anticancer agents: a patent review (2007 – 2010)

Background: Cancer is one of the major causes of worldwide human mortality. A number of existing antineoplastic medications and treatment regimens are already working in the field and several new compounds are in different phases of clinical trials. An extensive series of anticancer drugs exists in the market, and studies suggest that these molecules are associated with different types of adverse side effects. Reduction of the cytotoxicity of drugs to the normal cells is a major problem in anticancer therapy. Therefore, researchers around the globe are involved in the development of more efficient and safer anticancer drugs. The output of extensive research is that the quinazoline scaffold and its various derivatives can be explored further as a novel class of cancer chemotherapeutic agents that has already shown promising activities against different tumours. Quinazoline derivatives have already occupied a crucial place in modern medicinal chemistry.Various research has been performed on quinazoline and their derivatives for anticancer activity and pharmacological importance of this scaffold has been well established. Objective: The aim of this review is to compile and highlight the developments concerning the anticancer activity of quinazoline derivatives as well as to suggest some new aspects on the expansion of anticancer activity of novel quinazoline derivatives as anticancer agents in the near future. Methods: Recent literature related to quinazoline derivatives endowed with encouraging anticancer potential is reviewed. With special focus on quinazoline moiety, this review offers a detailed account of multiple mechanisms of action of various quinazoline derivatives: inhibition of the DNA repair enzyme system, inhibition of EGFR, thymidylate enzyme inhibition and inhibitory effects for tubulin polymerization by which these derivatives have shown promising anticancer potential. Results: Exhaustive literature survey indicated that quinazoline derivatives are associated with properties of inhibiting EGFR and thymidylate enzyme. It was also found to be involved in disturbing tubulin assembly. Furthermore, quinazoline derivatives have been found to inhibit critical targets such as DNA repair enzyme. These derivatives have shown significant activity against cancer. Conclusion: In cancer therapy, Quinazoline derivatives seems to be quite promising and act through various mechanisms that are well established. This review has shown that quinazoline derivatives can further be explored for the betterment of chemotherapy. A lot of potential is still hidden which demands to be discovered for upgrading quinazoline derivatives efficacy.

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Potential Anticancer Agents. I. Synthesis of Isoxazole Moiety Containing Quinazoline Derivatives and Preliminarily in vitro Anticancer Activity

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520614666140812105445 ◽

2014 ◽

Vol 15 (1) ◽

pp. 131-136 ◽

Cited By ~ 12

Author(s):

Jian-Ping Yong ◽

Can-Zhong Lu ◽

Xiaoyuan Wu

Keyword(s):

Anticancer Activity ◽

Anticancer Agents ◽

Quinazoline Derivatives

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Discovery, Development, Inventions, and Patent Trends on Mobocertinib Succinate: The First-in-Class Oral Treatment for NSCLC with EGFR Exon 20 Insertions

Biomedicines ◽

10.3390/biomedicines9121938 ◽

2021 ◽

Vol 9 (12) ◽

pp. 1938

Author(s):

Mohd Imran ◽

Shah Alam Khan ◽

Mohammed Kanan Alshammari ◽

Meshal Ayedh Alreshidi ◽

Abeer Abdullah Alreshidi ◽

...

Keyword(s):

Anticancer Agents ◽

Oral Treatment ◽

Growth Factor Receptor ◽

Lung Cancers ◽

Patent Review ◽

Patent Literature ◽

Patent Applications ◽

Exon 20 ◽

Nsclc Patients ◽

Process Composition

The majority of lung cancers are non-small-cell lung cancer (NSCLC) having a low survival rate. Recent studies have indicated the involvement of epidermal growth factor receptor (EGFR) oncogene mutations like EGFR exon 20 insertions (EGFRex20ins) mutation among NSCLC patients. The response of patients of NSCLC with the EGFRex20ins mutation to the currently available EGFR inhibitor is negligible. Mobocertinib is the first oral treatment that has been approved by the USFDA, on 15 September 2021, to treat NSCLC with the EGFRex20ins mutation. This patent review discusses the inventions and patent literature of mobocertinib that will help the scientific community to develop additional and improved inventions related to mobocertinib. The structure of mobocertinib was first reported in 2015. Therefore, this article covered the patents/patent applications related to mobocertinib from 2015 to 25 October 2021. The patent search revealed 27 patents/patent applications related to compound, method of treatment, salt, polymorph, process, composition, and drug combinations of mobocertinib. The authors foresee an exciting prospect for developing a treatment for NSCLC with EGFRex20ins mutation, and other cancers employing a combination of mobocertinib with other approved anticancer agents. The inventions related to novel dosage forms, processes, and intermediates used in the synthesis of mobocertinib are also anticipated.

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