Author(s): Kavitha K, Srinivasan N, Mohan S, Suresh R

Email(s): kavithakrocks@gmail.com

DOI: 10.52711/0974-360X.2021.00842   

Address: Kavitha K1*, Srinivasan N2, Mohan S1, Suresh R2
1Department of Pharmaceutical Chemistry, Karpagam College of Pharmacy, Ottakalpandapam, Coimbatore, Tamil Nadu.
2Department of Pharmacy, Faculty of Engineering and Technology, Annamalai University, Annamalai Nagar, Tamil Nadu.
*Corresponding Author

Published In:   Volume - 14,      Issue - 9,     Year - 2021


ABSTRACT:
Epidermal growth factor receptor (EGFR) acting very important part in cell growth regulation, one of the most significant consideration studied targets of tyrosine kinases (TK) inhibitors. A number of TKs take component in the role cell proliferation, differentiation and metastasis, survival and tolerant activation by mechanisms for instance point mutation might show the way to huge proportion of clinical cancers. EGFR is in excess articulated within many tumors, as well as ovarian, breast and bladder, head, brain, prostate, lung tumors. based in the field of literature study found that the invention of quinazolin 4(3H) one derivatives of structural modifications which produce their potential of cytotoxic properties. By inhibit the EGFR-TKs enzyme. In this, we introduced newly synthesized quinazolinones compounds to systematically investigate binding affinity and drug likeliness property against EGFR-TKs. the interaction of newly synthesized molecules QOC1-QOC6 against 1M17 Protein five derivatives of quinazolinone an induced fit docking analysis indicated are involved in binding affinity. The present study aimed at studies showed with the systematic analysis, the newly synthesized potential quinazolinone are recommended so as to these molecules would provide the same as enhanced show the way lead moiety for cytotoxic activity.


Cite this article:
Kavitha K, Srinivasan N, Mohan S, Suresh R. Insilco Design and Potential Cytotoxic agents EGFR Inhibitors of 4(3H) Quinazolinone Derivatives. Research Journal of Pharmacy and Technology. 2021; 14(9):4849-5. doi: 10.52711/0974-360X.2021.00842

Cite(Electronic):
Kavitha K, Srinivasan N, Mohan S, Suresh R. Insilco Design and Potential Cytotoxic agents EGFR Inhibitors of 4(3H) Quinazolinone Derivatives. Research Journal of Pharmacy and Technology. 2021; 14(9):4849-5. doi: 10.52711/0974-360X.2021.00842   Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2021-14-9-56


REFERENCES:
1.    Ugi I, Domling A and Werner B, J Heterocyclic Chem., 2000; 37: 647.
2.    Shirakawa S and Kobayashi S, Org Lett. 2006; 8: 4939-4942.
3.    Kavitha K, Srinivasan N, Haribabu A Review on quinazolinone and its derivatives with diverse biological activities. World Journal of Pharmacy and Pharmaceutical Sciences.2017; 7(4): 628-64.
4.    Yarden Y, Sliwkowski MX, Untangling the ErbB signaling network. Nature review molecular cell biology. 2001; 2: 127-137.
5.    Carpenter G, Cohen S. Epidermal growth factor. Annu Rev Biochem, 1979; 48: 193-216.
6.    Herbst RS, Langer CJ, Epidermal growth factor receptors as a target for cancer treatment. The emerging role of IMC-C225 in the treatment of lung and head and neck cancer. Semin Oncol. 2002; 29: 27-36.
7.    Salomon DS, Brandt R, Ciardiallo F, et al, Epidermal growth factor related peptides and their receptors in human malignancies. Crit Rev Oncol Hematol. 1995; 19: 183-232.
8.    Mendelsohn J, Dinney CP. The Willet F. Whitmore, Jr, lectureship. Blockade of epidermal growth factor receptors as anticancer therapy. Urol 2001; 165: 1152-1157.
9.    Yi Le, YIyuan Gan et al, Design, synthesis and in vivo biological evaluation of quinazolinone derivatives as EGFR inhibitors for anti tumor treatment. Journal of Enzyme Inhibition and Medicinal Chemistry. 2020; 35(1): 555-564.
10.    Lipinski CA, Lombardo F, Dominy BW, Feeney PJ. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Rev. 2001; 46(1-3): 3-26.
11.    Jeffrey R, Deschamps the role of crystallography in drug design. The AAPS Journal.E813-E819.
12.    James R. Connolly, Introduction to X-ray powder diffraction, Spring, 2012.
13.    Morris G M, Huey R, Lindstrom W, Scanner M F, Belew R K, Good sell D S and Olson A J Auto dock 4 and Auto dock tools4: Automated docking with selective receptor flexibility J. Comput. Chem. 2009; 30: 2785
14.    Srivastava V, Kumar A. Molecular Docking Studies on DMDP Derivatives as human DHFR inhibitors. Bioinformation. 2008; 3(4): 180-188.
15.    Daidon, G.et al, Synthesis and pharmacological study of ethyl 1-methyl-5-(substituted 3, 4-dihydro-4 oxo quinazolin-3-yl)-1H-Pyrazole-4-acetates. European Journal of Medicinal Chemistry. 2001:36:737.
16.    El-Meligic S, et al, Microwave assisted synthesis of quinazolinone using different bases. J. Chem (sec B). 2001; 40: 62.
17.    KK. Rajasekhar, ND Nizamuddin Abdrrahman Shemsu Surur, Yennus Tadesse Mekonnen synthesis characterization, anti tubercular and antibacterial activity and molecular docking of 2,3-di substituted quinazolinone derivative. Research and Reports in Medicinal Chemistry. 2016; 6: 15-26.
18.    Sako Mirzaie, Majid Monajjemi, Mohammad Sajeed Hakhamaneshi, Fardin Fathi, Mustafa Jamalan. Combined 3D QSAR on Multi Acting quinazoline derivatives as HER2 Kinase inhibitors. EXCLI Journal, 2013; 12: 130-143.
19.    Molinspiration Cheminformatics, Bratislava, Slovak Republic, Available from, Molinspiration.com/services/properties.html (accessed 16.08.2010).
20.    Zhao Y, Abraham MH, Lee J, Hersey A, Luscombe NC, Beck G, Sherborne BI. Rate-limited steps of human oral absorption and QSAR Studies Pharm. Res .2002; 19: 1446-1456.
21.    Osman M, O. Habib, Hussein M, Hassan, Ahmed El-Mekabaty, studies on some benzoxazine-4-one derivatives with potential biological activity. American Journal of Organic Chemistry 2012; 2(3): 45-51.

Recomonded Articles:

Research Journal of Pharmacy and Technology (RJPT) is an international, peer-reviewed, multidisciplinary journal.... Read more >>>

RNI: CHHENG00387/33/1/2008-TC                     
DOI: 10.5958/0974-360X 

1.3
2021CiteScore
 
56th percentile
Powered by  Scopus


SCImago Journal & Country Rank


Recent Articles




Tags


Not Available