ABSTRACT:
Imidazole, thiazole, and oxadiazoles, which are substituted five-member rings, appear to have a promising function in a variety of activities. Because of their many significant scientific and therapeutic uses, oxadiazole is a special class of heterocycles that has been created as antibacterial, anti-cancer, and anti-inflammatory compounds. As a result, they have been found to be inhibitors of various enzymes, receptor modulators, and neuroprotective medications. The goal of this study was to precisely design oxadizole derivatives that had the potential to inhibit thymidine phosphorylase in order to synthesize oxadiazole derivatives using the resources at hand. Additionally, the study aimed to synthesize and characterize oxadizoles and assess their ability to inhibit thymidine phosphorylase in malignant cells using invitro enzymes. Finally, an overall comparison of the insilico and invitro inhibiting potential of oxadiazoles
Cite this article:
Dr. Sundhararajan, Seraphine Joyce J, Gopinath C, Gowtham B, Guruprasath. R. Oxadiazoles-Insimulation to repercussion in malignancy. IJRPAS, March 2025; 4 (3): 43-49.DOI: https://doi.org/https://doi.org/10.71431/IJRPAS.2025.4306
2. Davinder,K.;
Virender,K.; Rakesh ,M.; Gajendra, S.Oxadiazole-an Important Bioactive Scaffold
for Drug Discovery and Development Process against HIV and Cancer—AReview.
Curr. Bioact. Compd. 2019,15,271–279.
3.
Toi M, Rahman MA, Bando H, Chow LW (2005 )
Thymidine phosphorylase (platelet-derived endothelial growth factor) in cancer
biology and treatment. Lancet Oncol 6(3):158–166)
4. Sebastian
Salentin, V Joachim Haupt, Simone Daminelli, Michael Schroeder. Progress in
biophysics and molecular biology 116 (2-3), 174-186, 2014.
5. Murali Ararthy, Sanjeev Kumar Singh
. Advances in protein molecular and structural biology methods 2022
6. Sebastian
Salentin, V Joachim Haupt, Simone Daminelli, Michael Schroeder. Nucleic acids
research 43(W1), W443-W447,2015
7. Sree Karani kondapuram, Sailu
sarvagalla, Mohane selvaraj Coumar Molecular Docking for Computer-aided Drug Design
, 463-477, 2021
8.
SivridisE,GiatromanolakiA,KoukourakisMI,BicknellR,HarrisAL,GatterKC(2000)
Thymidine phosphorylase expression in normal and hyper plastic endometrium.J
ClinPathol53(9):704–708
9.
Zhang L, Mackenzie IZ, Rees MC, Bicknell R
(1997) Regulation of The expression of the angiogenic enzyme platelet-derived
endothelial cell growth factor /thymidine phosphorylase in endometrial isolates
by ovarian steroids and cytokines.
10. Tiwari,A.,GopalanKutty,N.,Kumar,N.,Chaudhary,A.,VasanthRaj,P.,Shenoy,R.,&Mallikarjuna
Rao, C. (2016).
Synthesisandevaluationofselected1,3,4-oxadiazolederivativesforinvitro
cytotoxicity and in vivo anti- tumor activity.
11. Benassi,Alessandra,FilippoDoria,andValentinaPirota.
“Ground breaking anticancer Activity of highly diversified oxadiazole
Scaffolds.
12. k.Shanmugam,SrishtiMishra,ArunachalamChinnathambi,SulaimanAliAlharbieta
"Novel1,3,4-oxadiazole induces anticancer activity by targeting NF-κB in
hepatocellular carcinoma cells
13. Subramanyam, M., Sreenivasulu, R., Gundla,R.,
Rao, M.V. and Rao, K.P., 2018. Synthesis, Biological evaluation and docking
studies of 1,3,4-oxadiazole fused benzothiazole Derivatives for anticancer
drugs
14. DeOliveira,
C.S.;Lira, B.F.;Barbosa-Filho, J.M.; Lorenzo, J.G.F.; deAthayde-Filho,
P.F.Synthetic Approaches and P harmacological Activity of 1,3,4-Oxadiazoles :A
Review of the Literature from 2000 2012.Molecules 2012, 17, 10192–10231
15. DavinderKumar,
Navidha Aggarwal , Aakash Deep, HarshKumar, HiteshChopra, 63 Rakesh Kumar
Marwaha , and Simona Cavalu An Understanding of Mechanism-Based Approaches for
1,3,4-Oxadiazole Scaffolds as Cytotoxic Agents and Enzyme Inhibitors, .
Pharmaceuticals2023, 16, 254.https://doi.org/10.3390/ph16020254