Third Generation EGFR Inhibitors: Overcoming EGFR Resistance and Toxicity Problems reviews current issues relating to the design of reversible and irreversible third generation EGFR inhibitors, highlighting the types of mutation responsible for resistance, and providing different chemical starting points for researchers to optimize and develop in designing the next generation of drugs. Beginning with an introduction to EGFR inhibitors and a review of inhibitors currently approved or in clinical trials, the book goes on to discuss current approaches in the development of both covalent irreversible and covalent reversible EGFR Inhibitors. In addition, mechanisms of resistance to third generation inhibitors, and discovery of fourth generation allosteric C797S inhibitors are explored before a discussion of potential future trends.
This comprehensive coverage of the design and development of improved analogues to overcome the problems of resistance and toxicity associated with third generation EGFR inhibitors makes Third Generation EGFR Inhibitors a crucial resource for medicinal chemists, drug developers, and researchers investigating cancer therapeutics.
- Includes full synthetic schemes of all approved and in-trial third generation inhibitors
- Highlights the emergence of fourth generation EGFR inhibitors and the possibilities of them overcoming constraints of third generation compounds
- Provides a structural correlation of third and fourth generation EGFR inhibitors, reviewing both their design strategies and typical anticancer activity
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1. Introduction 2. Approved and Clinical Trial Third Generation EGFR inhibitors 3. Current approaches in the development of Covalent Irreversible EGFR Inhibitors 4. Current approaches in the development of Covalent Reversible EGFR Inhibitors 5. Mechanism of Resistance to Third Generation Inhibitors 6. Discovery of Fourth Generation Allosteric C797S Inhibitors 7. Conclusion and Future Perspectives
Harun Patel is an Associate Professor in the Division of Computer Aided Drug Design, at the R. C. Patel Institute of Pharmaceutical Education and Research's Dept. of Pharmaceutical Chemistry. In addition to being the recipient of multiple awards, Dr Patel has over 70 publications in reputed peer reviewed international journals (which have achieved over 600 citations), three international books, and two patents to his name. His key research interests involve QSAR, docking studies, virtual screening, and synthesis of novel anticancer, anti-tubercular and antiepileptic drugs.
Rahul Pawara is an Associate Professor in the Division of Computer Aided Drug Design, at the R. C. Patel Institute of Pharmaceutical Education and Research's Dept. of Pharmaceutical Chemistry, which he joined following two years of work as a Field Officer in an ICMR-funded project studying Tuberculosis in tribal areas. He has five international publications in peer reviewed journals, and his main research interest is the design and synthesis of novel anti-cancer agents.
Surana, Sanjay J.