Author(s): Satvir Singh, Divya. D. Bhandari, Monika Gupta, Jagdeep Singh

Email(s): divya.pharma@cumail.in

DOI: 10.52711/0974-360X.2022.00738   

Address: Satvir Singh1, Divya. D. Bhandari1, Monika Gupta2, Jagdeep Singh3
1University Institute of Pharmaceutical Sciences, Chandigarh University, Gharuan, Mohali, Punjab, India.
2Department of Pharmaceutical Chemistry, Amar Shaheed Baba Ajit Singh Jujhar Singh Memorial College of Pharmacy, Bela, Ropar, Punjab, India.
3Indian Institute of Technology, Ropar, Punjab, India.
*Corresponding Author

Published In:   Volume - 15,      Issue - 10,     Year - 2022


ABSTRACT:
A total of 18 derivatives S(1-18) of naphthoic acid linked Imidazo[2,1-b][1,3,4]thiadiazole were synthesized and tested for their anticancer potential at human cancer cell line A – 549. The interaction of the proposed derivatives with the colchicine binding domains of the receptor was also performed using Maestro 10.5 program (Schrodinger Inc. USA). Molecular docking study was performed for synthesized compounds displaying a significant inhibitory activity in order to validate their binding mode to active site. All the 18 inhibitors were docked into the active site of the receptor in two poses. The G-scores and binding energy for compound S4, S10, S12, S13 and S16 were observed to be comparable to the standard Colchicine. The compound S1, S5, S10, S12 and S16 exhibited prominent inhibition of cancer cell line.


Cite this article:
Satvir Singh, Divya. D. Bhandari, Monika Gupta, Jagdeep Singh. Design, Synthesis and Anticancer potential evaluation of Novel Naphthoic Acid linked Imidazo[2,1-b][1,3,4]thiadiazoles. Research Journal of Pharmacy and Technology2022; 15(10):4405-2 doi: 10.52711/0974-360X.2022.00738

Cite(Electronic):
Satvir Singh, Divya. D. Bhandari, Monika Gupta, Jagdeep Singh. Design, Synthesis and Anticancer potential evaluation of Novel Naphthoic Acid linked Imidazo[2,1-b][1,3,4]thiadiazoles. Research Journal of Pharmacy and Technology2022; 15(10):4405-2 doi: 10.52711/0974-360X.2022.00738   Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2022-15-10-11


REFERENCES:
1.    Jangde R. An Overview of Researched Erthyrocyte for Cancer therapy. Asian Journal of Research in Pharmaceutical Sciences. 2011; 1(4): 83-92. DOI: 10.5958/2231-5659.
2.    Saha D. Maity T. Jana M. Mandal S. Cancer treatment strategy- An Overview. Asian Journal of Pharmaceutical Technology. 2011; 1(2):28-33. DOI: 10.5958/2231–5713.
3.    Nag M K. Patel S. Panik R. Shirvastava S. Daharwal S J. Singh M R. Singh D. Lung Cancer Targeting: A Review. Research Journal of Pharmacy and Technology. 2013; 6(11): 1302-1306. DOI: 10.5958/0974-360X
4.    Anand P. Kunnumakkara A B. Cancer is a preventable disease that requires major lifestyle changes. Pharmaceutical Research. 2008, 25, 2097-2116. http://dx.doi.org/10.1007/s11095-008-9690-4.
5.    Saha D. Tamrakar A. Jana M. Mandal S. Skin Cancer: Dance of death. Asian Journal of Pharmaceutical Research. 2011; 1(2): 34-36. DOI: 10.5958/2231–5691.
6.    Hameed S A. Varkey J. Jayashekhar P. Schiff bases and bicyclic derivatives comprising 1,3,4- thiadiazole moiety- A review on their pharmacological activities. Asian Journal of Pharmaceutical Research.2019; 9(4): 299-306. DOI:10.5958/2231-5691.2019.00047.9
7.    Ranjith US. Muhammed S. Molecular docking study of Novel Imidazo[2,1-b][1,3,4] thiadiazole derivatives. Research Journal of Pharmacy and Technology. 2013; 6(6): 688-694. DOI: 10.5958/0974-360X
8.    Girija K. Jamuna B. Design and synthesis of some novel schiff’s base aryl imidazole derivatives, characterization, docking and study of their antimicrobial activity. Research Journal of Pharmacy and Technolgy. 2015; 8(4): 407-415. DOI: 10.5958/0974-360X.2015.00069.4.
9.    Sindhu T J. Arathi K N. Devi A. Aswathi T A. Noushid M. Kuttiyil S S. Synhtesis,molecular docking and antibacterial studies of novel azole derivatives as enoyl ACP reductase inhibitor in E. coli. Asian Journal of Research in Pharmaceutical Sciences. 2019; 9(30: 174-180. DOI: 10.5958/2231-5659.2019.00027.4
10.    Gadad A K. Mahajanshetti C S. Nimbalkar S. Raichurkar A. Synthesis and antibacterial activity of some 5-guanylhydrazone/thiocyanato-6-arylimidazo [2,1-b][1,3,4]thiadiazole-2-sulfonamide derivatives. European Journal of Medicinal Chemistry. 2000; 35: 853-859. DOI: 10.1016/s0223-5234(00)00166-5.
11.    Basedia DK. Shrivastava B. Dubey B K. Sharma P. Synthesis and anticancer activity of novel substituted 1,3,4-oxadiazolo- [3,2-a]- 1,3,5- triazine and 1,3,4- thiadiazole-[3,2-a]- 1,3,5- trizazine derivatives. Asian Journal of Research in Chemistry. 2014; 7(3): 310-315. DOI: 10.5958/0974-4150.
12.    Zheng S Y. Li y. Jiang D. Zhar J. Ge JF. Anticancer effect and apoptosis induction by quercetin in the human lung cancer cell line A-549. Molecular Medicine Reports.2012; 5: 822-826. DOI: 10.3892/mmr.2011.726.
13.    Kalkotwar R S. Saudagar R B. Design, synthesis and anti-microbial, anti – inflammatory, anti – tubercular activities of some 2,4,5 tri tri substituted imidazole derivatives. Asian Journal of Pharmaceutical Research. 2013; 3(4): 159-165. DOI: 10.5958/2231–5691.
14.    Saini R. Rai A K. Kesari A N. Yar M S. Synhtesis and biological evaluation of 2,5- disubstituted 1,3,4 oxadiazoles. Asian Journal of Research in Chemistry. 2009; 2(1): 34- 36. DOI: 10.5958/0974-4150.


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

Journal Policies & Information


Recent Articles




Tags


Not Available