Synthesis and evaluation of thiazolidinone–pyrazole conjugates as anticancer and antimicrobial agents

Author:

Bhat Mahima1,Poojary Boja1,Kalal Bhuvanesh Sukhlal23,Gurubasavaraja Swamy Purawarga Matada4,Kabilan Senthamaraikannan5,Kumar Vasantha6,Shruthi Nooji1,Alias Anand Selvam Athavan5,Pai Vinitha Ramanath2

Affiliation:

1. Department of Chemistry, Mangalore University, Mangalagangothri-574199, Karnataka, India

2. Department of Biochemistry, Yenepoya Medical College, Yenepoya University, Mangaluru, Karnataka, India

3. Yenepoya Research Center, Yenepoya University, Mangaluru, Karnataka, India

4. Medicinal Chemistry Research Laboratory, Acharya & BM Reddy College of Pharmacy, Bangalore 560090, Karnataka, India

5. Drug Discovery Lab, Department of Chemistry, Annamalai University, Annamalainagar, Tamil Nadu 608002, India

6. Department of Chemistry, SDM College (Autonomous), Ujire-574240, Karnataka, India

Abstract

Aim: To synthesize a series of new thiazolidinone–pyrazole hybrids (5a–o) and assess their anticancer (in vitro and in vivo) and antimicrobial activities. Results: The compounds 5h (against Ehrlich ascites carcinoma cells), 5e and 5i (against the human breast cancer [MDA-MB231] cell line) exhibited potent anticancer activity. All the compounds except 5g and 5e found to be less toxic for the human dermal fibroblast cells. The effective interactions of the compounds in silico with MDM2 exemplified their inhibitory potency. The derivatives also showed moderate antimicrobial activity. Conclusion: The halogen atoms on various positions of the N-arylamino ring played an advantageous role in elevating the potency of the molecules. Thus, these conjugates could be used as a lead for further optimization to achieve promising therapeutics.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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