Sirassu Narsimhaa, Yellu Narasimha Reddyb, Vasudeva Reddy Nagavellia*
aDepartment of Chemistry Kakatiya University, Warangal, T. S. 506009, India
bDepartment of Pharmacology and Toxicology, Kakatiya University, Warangal, T. S. 506009, India
*Address for corresponding author
Dr. Vasudeva Reddy Nagavelli
Department of Chemistry, Kakatiya University, Warangal, T. S. 506009, India
Objective: Twenty five 1,2,3-triazole derivatives of phenothiazines (5a-5k, 6a-6g, and 7a-7g) were synthesized in order to evaluate their anti-proliferative and antibacterial activities. Material and methods: The newly synthesized compounds were characterized by spectroscopic (FTIR, 1H NMR, 13C NMR and Mass) analysis after synthesis. All compounds were screened for their in vitro anticancer activity against MCF-7 (breast), HeLa (cervical) and A-549 (alveolar) cell lines. The minimum inhibitory concentrations (MIC) of the synthesized compounds (5a-5k, 6a-6g and 7a-7g) were tested against the gram-positive organisms B. subtilis, S. aureus and S. epidermidis and the gram-negative organisms E. coli, P. aeruginosa, and K. pneumoniae. Results: The in vitro cytotoxic examination results revealed that compounds 7a and 7b exhibited good anti-proliferative activity against three cancer cell lines, MCF-7, HeLa and A-549 with IC50 values ranging from 09.11 ± 0.3 µM to 20.11 ± 1.0 µM respectively. Antibacterial activity revealed that the compounds 5d, 6d, and 7d against B. subtilis and S. aureus, compound 5i against P. aeruginosa and compound 5j against E. coli and P. aeruginosa have shown equipotent activity on comparing with the standard drugs penicillin and streptomycin. Conclusion: We succeeded in guiding the change of substituents in the triazole ring together with the phenothiazine-5,5-dioxide group, which played a crucial role in the development of a promising anticancer activity and also shown equipotent antibacterial activity against gram-positive and gram-negative organisms. By making a simple modification of the structure, a new potent analog having the desired anticancer and antibacterial activity can be produced with good efficiency.
Keywords: Phenothiazine, 1, 2, 3-triazole, anticancer activity, antibacterial activity