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Vol. 36 No. 12 (2024): Vol 36 Issue 12, 2024

Copyright (c) 2024 Premanand M. Honavar, Bhuvanesh Sukhlal Kalal, Ranjith Raj, Anjana P.T. , Deepthi P.V., Sharatha Chandra, Vijesh A. M. , Ramith Ramu, Vinitha Ramanatha Pai, Naveen Kumar, Vasantha Kumar, B. Shivarama Holla

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Thiazolyl-Thiazolidinone Conjugated Pyrazoles as Potential Anticancer and Antibacterial Agents and Molecular Docking Studies

https://doi.org/10.14233/ajchem.2024.32708
Premanand M. Honavar
Department of Chemistry, Sri Dharmasthala Manjunatheshwara College of Arts, Science, Commerce, Honavar-581334, India; Department of Chemistry, Tumkur University, Tumkur-572103, India
https://orcid.org/0000-0002-8182-6220
Bhuvanesh Sukhlal Kalal
Department of Biochemistry, Yenepoya Medical College, Yenepoya (Deemed to be University), Deralakatte, Mangaluru-575018, India; Department of Pharmacology and Nutritional Sciences, College of Medicine, University of Kentucky, Lexington, Kentucky 40508, USA
https://orcid.org/0000-0002-2560-3778
Ranjith Raj
Department of Pharmacology, JSS Medical College, JSS Academy of Higher Education and Research, Mysuru-570015, India
https://orcid.org/0009-0009-0073-1341
P.T. Anjana
Department of Chemistry, Krishna Menon Memorial Government Women’s College (Affiliated to Kannur University), Pallikkunnu, Kannur-670004, India
https://orcid.org/0009-0007-5251-6403
P.V. Deepthi
Department of Chemistry, Nehru Arts and Science College (Affiliated to Kannur University), Kanhangad-671314, India
https://orcid.org/0009-0006-2491-9531
Sharatha Chandra
Department of Biosciences, Mangalore University, Mangalagangothri-574199, India
https://orcid.org/0009-0002-8755-5430
A.M. Vijesh
P.G. Department of Chemistry, Payyanur College (Affiliated to Kannur University), Payyanur-670327, India
https://orcid.org/0009-0003-4250-2391
Ramith Ramu
Department of Biotechnology and Bioinformatics, School of Life Sciences, JSS Academy of Higher Education and Research, Mysuru-570015, India
Vinitha Ramanatha Pai
Department of Biochemistry, Yenepoya Medical College, Yenepoya (Deemed to be University), Deralakatte, Mangaluru-575018, India
https://orcid.org/0000-0003-0893-3369
Naveen Kumar
1Department of PG Studies and Research in Chemistry, Sri Dharmasthala Manjunatheshwara College (Autonomous), Ujire-574240, India
https://orcid.org/0000-0003-4663-0246
Vasantha Kumar
Department of PG Studies and Research in Chemistry, Sri Dharmasthala Manjunatheshwara College (Autonomous), Ujire-574240, India
https://orcid.org/0000-0002-8915-5847
B. Shivarama Holla
Department of PG Studies and Research in Chemistry, Sri Dharmasthala Manjunatheshwara College (Autonomous), Ujire-574240, India
https://orcid.org/0009-0003-0531-4850

Corresponding Author(s) : Vasantha Kumar

vasantha.kumar1886@gmail.com

Asian Journal of Chemistry, Vol. 36 No. 12 (2024): Vol 36 Issue 12, 2024

Abstract

In current study, five new compounds containing thiazolyl-thiazolidinone conjugated substituted pyrazoles were prepared and screened for anticancer and antimicrobial activities. Synthesized compounds were characterized by spectroscopic techniques. Anticancer activity was carried out against human melanoma cancer A375 and human breast cancer MDA-MB-231 cell lines. Also, these were screened for antibacterial activity against two Gram-positive Staphylococcus aureus, Bacillus subtilis strains and three Gram-negative Pseudomonas aeruginosa, Klebsiella pneumonia and Escherichia coli strains. Anticancer studies have identified compound 6e as highly potent compound with IC50 = 13.08 µg/mL against A375 cell line and 14.21 µg/mL against MDA-MB-231 cell line. In addition, compound 6c also showed very good activity against A375 cell line with IC50 = 13.22 µg/mL. Antibacterial activity results revealed compound 6a and 6e as highly promising agents against all the tested bacterial strains which is equipotent to the standard drug. Molecular docking studies on Aurora A kinase also revealed favourable interactions for target compounds through hydrogen bonds.

Keywords

Thiazolidinones Pyrazoles Anticancer activity Antibacterial activity Docking studies Aurora A kinase
Honavar, P. M., Kalal, B. S., Raj, R., Anjana, P., Deepthi, P., Chandra, S., … Holla, B. S. (2024). Thiazolyl-Thiazolidinone Conjugated Pyrazoles as Potential Anticancer and Antibacterial Agents and Molecular Docking Studies. Asian Journal of Chemistry, 36(12), 2855–2860. https://doi.org/10.14233/ajchem.2024.32708
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