Author(s):
Meghna H. Seta, Monika T. Kyada
Email(s):
patel.meghna287@gmail.com
DOI:
10.52711/0974-360X.2025.00529 
Address:
Meghna H. Seta1*, Monika T. Kyada2
1Department of Pharmaceutical Sciences, Faculty of Health Sciences, Marwadi University, Rajkot - Morbi Highway, Rajkot, Gujarat, India - 360 003.
2C.K. Pithawalla Institute of Pharmaceutical Science and Research, Surat, Gujarat, India - 395 007.
*Corresponding Author
Published In:
Volume - 18,
Issue - 8,
Year - 2025
ABSTRACT:
We designed and synthesized newer heterocyclic compounds with 1, 3, 4-thiadiazole, pyrimidine, and 1, 3, 4 -oxadiazole, with aimed to develop Histone Deacetylase (HDAC) inhibitors. The 1, 3, 4 - oxadiazole nucleus known for its diverse pharmacological properties and incorporating the thiadiazole and pyrimidine groups. The progress of synthesis was monitored using Thin Layer Chromatography (TLC). Further products were confirmed by IR, Mass spectra, melting point, IR and 1H-NMR. A molecular docking study indicated that synthesized compounds have great HDAC inhibitory activity. The biological evaluation of one derivative, compound VIII (a) was performed by the MTT assay, revealed notable anti-cancer activity. These findings suggest that the novel 1, 3, 4 - oxadiazole compounds could serve as promising candidates for futuristic development of anti-cancer agents.
Cite this article:
Meghna H. Seta, Monika T. Kyada. Design, Synthesis and Anti Cancer Evaluation of novel 1, 3, 4-oxadiazoles. Research Journal Pharmacy and Technology. 2025;18(8):3677-3. doi: 10.52711/0974-360X.2025.00529
Cite(Electronic):
Meghna H. Seta, Monika T. Kyada. Design, Synthesis and Anti Cancer Evaluation of novel 1, 3, 4-oxadiazoles. Research Journal Pharmacy and Technology. 2025;18(8):3677-3. doi: 10.52711/0974-360X.2025.00529 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2025-18-8-32
REFERENCES:
1. Goyal RK. In Elements of Pharmacology, B. S. Shah Prakashan, 21st ed., pp. 588-592, 2012-2013.
2. Rutuja Sawant, Aloka Baghkar, Sanjukta Jagtap, Lina Harad, Anagha Chavan, Nilofar A. Khan, Rupali P. Yevale, Mohan K. Kale. A Review on - Herbs in Anticancer. Asian J. Res. Pharm. Sci. 2018; 8(4): 179-184.doi: 10.5958/2231-5659.2018.00031.0
3. Amiza, Abdul Rauf, Ayesha Mohy ud Din, Fatima Ahmad, Saira Sehar, Adeel Ahmad Khawaja, Shah Muhammad Haroon, Rehana Iqbal. A Concise Review on Toxicity and Pharmacological Aspects of Foeniculum vulgare with Emphasis on Anti-Cancer Potential. Asian Journal of Research in Pharmaceutical Sciences. 2022; 12(1): 75-2. doi: 10.52711/2231-5659.2022.00013
4. Pankaj B. Bhogam, Sushant A. Gharal, Tushar B. Patil, Aarti A. Varne, Priyanka S. Lad. A Systematic Review on Anticancer Phytosomal Flavonoids. Asian Journal of Research in Pharmaceutical Sciences. 2023; 13(4): 343-6. doi: 10.52711/2231-5659.2023.00059
5. Prakash S. Sukhramani, G. Vidyasagar, Piyush M. Patel. In-vitro screening of Ficus racemosa for Anticancer activity. Research J. Pharmacognosy and Phytochemistry. 2013; 5(3): 119-122.
6. Mayur Poddar, Tejraj M. Aminabhavi, Malleshappa N. Noolvi and Meghna Patel. HIF Inhibitors: New Hope for Cancer Therapy. Letters in Drug Design and Discovery. 2015; 12: 01-18. doi: 10.2174/1570180812666150414214938
7. Sharma S, Sharma PK, Kumar N and Dudhe R. A Review: Oxadiazole their chemistry and pharmacological potentials. Scholars Research Library, Der Pharma Chemica, 2010; 2: 253-263.
8. Prabhu C Jalihal, Suresh Sharabsappa, Basavaraj Kilarimath. Synthesis and Antimicrobial Activity of Some New 2, 5-Disubstituted 1, 3, 4-Oxadiazoles. Asian J. Research Chem. 2010; 3(2): 319-323.doi: 10.5958/0974-4150
9. Kaur H, Kaur H, Chawla P, Chawla A, Baghel US. A review on Chemistry and Biological Activities of Thiadiazole Derivatives. Am. J. Pharmatech. Res. 2014; 41: 214-233. doi: 10.1111/cbdd.12125
10. Ajay A. Kharche, Shriram H. Bairagi, Nilesh K. Gorde, Sachin S. Laddha. 1,3,4-Oxadiazole: A New Profile of Biological Activities. Asian J. Research Chem. 2011; 4(1): 1-12.
11. Chhama Shukla, Sanchit Srivastav. Biologically Active Oxadiazole. Asian J. Res. Pharm. Sci. 2015; 5(4): 227-233. doi: 10.5958/2231-5659.2015.00033.8
12. B.H. Kilarimath, V.G. Digge, S.S. Honnali, R.M. Sankangoud, P.C. Jalihal, Sonjoy Mandal. Synthesis and Antimicrobial Activity of Some Novel 2, 5-Di substituted 1, 3, 4-Oxadiazole Derivatives. Asian J. Research Chem. 2011; 4(5): 766-769.
13. Nachiket S. Dighe, Pankaj Shinde, Harshali Anap, Sanjay Bhawar, Deepak S. Musmade. QSAR Study and Synthesis of some new 2, 5-disubstituted 1, 3, 4-oxadiazole derivatives as Anti-microbial and Anti-inflammatory Agents. Asian J. Pharm. Res. 2014; 4(4): 174-179.
14. Rajak H, Agarawal A, Parmar P, Thakor B, Veerasamy R, Sharma P, Kharya M. 2,5-Disubstituted-1,3,4-oxadiazole/thiadiazole as surface recognition moiety: Design and synthesis of novel hydroxamic acid-based histone deacetylase inhibitors. Bioorg. Med. Chem. Lett. 2011; 21: 5735-5738. doi: 10.1016/ j.bmcl.2011.08.022
15. Ruijter AJM, Van Gennip AH, Caron HN, Kemp S. Histone deacetylases (HDACs): characterization of the classical HDAC family. BioChem. J. 2003; 370: 737–749. doi: 10.1042/BJ20021321
16. Atodaria B, Thakor V, Hasani J, Bhayani F, Noolvi MN. Synthesis and anticancer activity of new optically active 1, 3, 4-thiadiazole derivatives acting as histone deacetylase inhibitors by rational approach. J. Med. Pharm. Allied Sci. 2014; 4: 1-12.
17. Ropero S, Esteller M. The role of histone deacetylases (HDACs) in human cancer. Mol. Oncol. 2007; 1: 19-25. doi: 10.1016/ j.molonc.2007.01.001
18. Johnstone RW. Histone-Deacetylase Inhibitors: Novel Drugs for the treatment of cancer. Nat. Rev. Drug. Discov. 2002; 1: 287-299. doi: 10.1038/nrd772
19. Mort JS. Histone deacetylase – a new target for suppression of cartilage degradation. Arthritis Res. Ther. 2005; 7: 155-156. DOI: 10.1186/ar1781
20. Marks PA. Histone deacetylase inhibitors: A chemical genetics approach to unders cellular function. Biochim. Biophys. Acta. 2010; 1799: 717-725. doi: 10.1016/j.bbagrm.2010.05.008
21. Dokmanovic M, Clarke C, Marks PA. Histone Deacetylase Inhibitors: Overview and Perspectives. American Asso. Cancer Res. 2007; 5: 981-989.doi: 10.1158/1541-7786.MCR-07-0324
22. Vishwajit S. Patil, Prithviraj A. Patil. Molecular Docking: A useful approach of Drug Discovery on the Basis of their Structure. Asian Journal of Pharmaceutical Research. 2023; 13(3): 191-5. doi: 10.52711/2231-5691.2023.00036
23. Codd R, Braich N, Liu J, Soe CZ, Pakchung AH. Zn (II)-dependent histone deacetylase inhibitors: Suberoylanilidehydroxamic acid and trichostatin A. The International Journal of Biochemistry and Cell Biology. 2009; 41: 736-739. doi: 10.1016/j.biocel.2008.05.026
24. Vogel’s Textbook of Practical Organic Chemistry, 5th Ed., Longman Singapore Publishers Pvt. Ltd., 1258, 1996.
25. Patel K, Shah R, Javali V, Sreenivasa GM. Synthesis, Characterization and Anthelmintic Activity (PeritumaPosthuma) of New Oxadiazole Incorporated with Imidazole and Pyrazole. Int. J. Pharm. Bio Sci. 2010; 1: 1-13.
26. Gadad AK, Palkar MB, Anand K, Noolvi MN, Boreddy TS and Wagwade J. Synthesis and biological evaluation of 2-trifluoromethyl/sulfonamido-5,6- diaryl substituted imidazo[2,1-b]-1,3,4-thiadiazoles: A novel class of cyclooxygenase-2 inhibitors. Bioorg. Med. Chem. 2008; 16: 276-283. doi: 10.1016/j.bmc.2007.09.038
27. Petrini M and Torregiani E. Aza-Henry reaction of substituted nitroalkanes using a-formamidoaryl sulfones as N-acylimino equivalents. Tetrahedron Lett. 2006; 47: 3501-3503.
28. Suaad, Majidi MH and Al-Messri AK. Synthesis of some new substituted1, 2,4triazole and 1, 3, 4-thiadiazole and study of their activities on some strainsofbacteria. J. Al-Nahrain University. 2007; 10: 30-37. doi: 10.22401/JNUS.10.1.07