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Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using
Velma Ganga Reddy1, T Srinivasa Reddy2, Chetna Jadala3
1Academy of Scientific and Innovative Research (AcSIR), CSIR-Human Resource Development Centre (CSIR-HRDC) Campus, Ghaziabad, 201 002, Uttar Pradesh, India; Department of Organic Synthesis & Process Chemistry, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad, 500 007, India; Centre for Advanced Materials & Industrial Chemistry (CAMIC), School of Science, RMIT University, GPO Box 2476, Melbourne, 3001, Australia.
Abstract:
A series of new pyrazolo-benzothiazole hybrids (7-26) were synthesised and screened for their cytotoxic activity towards several cancer cell lines [colon (HT-29), prostate (PC-3), lung (A549), glioblastoma (U87MG)] and normal human embryonic kidney cell line (Hek-293T). Compounds 8, 9, 13, 14, 18, 19, 23, and 24 displayed significant activity, with compound 14 being particularly potent towards all the tested cancer cell lines with IC50 values in the range 3.17-6.77 μM, even better than reference drug axitinib (4.88-21.7 μM). Compound 14 also showed the strongest growth inhibition in 3D multicellular spheroids of PC-3 and U87MG cells. The mechanism of cellular toxicity in PC-3 cells was found to be cell cycle arrest and apoptosis induction through depolarisation of mitochondrial membrane potential, increased ROS production and subsequent DNA damage. Further, compound 14 displayed significant in vitro (VEGFR-2 inhibition) and in vivo [transgenic zebrafish Tg(flila:EGFP) model] antiangiogenic properties. Overall, these results provide strong evidence that compound 14 could be considered for a lead candidate in anticancer and antiangiogenic drug discovery.
Insights
Researchers developed new pyrazolo-benzothiazole compounds for cancer treatment. Compound 14 showed potent anticancer activity and antiangiogenic properties, making it a promising drug candidate.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Oncology
Background:
- Developing novel anticancer agents is crucial for effective cancer therapy.
- Pyrazolo-benzothiazole scaffolds have shown potential in drug discovery.
Purpose of the Study:
- To synthesize and evaluate novel pyrazolo-benzothiazole hybrids for cytotoxic and antiangiogenic activities.
- To identify potent anticancer drug candidates.
Main Methods:
- Synthesis of pyrazolo-benzothiazole hybrids (compounds 7-26).
- In vitro cytotoxicity screening against human cancer cell lines (HT-29, PC-3, A549, U87MG) and normal cells (Hek-293T).
- Assessment of antiangiogenic properties using VEGFR-2 inhibition and a zebrafish model.
Main Results:
- Compounds 8, 9, 13, 14, 18, 19, 23, and 24 exhibited significant cytotoxic activity.
- Compound 14 demonstrated potent anticancer effects across all tested cancer cell lines, outperforming the reference drug axitinib.
- Compound 14 induced cell cycle arrest and apoptosis in PC-3 cells and showed significant in vitro and in vivo antiangiogenic effects.
Conclusions:
- Compound 14 is a highly potent anticancer agent with significant antiangiogenic properties.
- This pyrazolo-benzothiazole derivative warrants further investigation as a lead candidate for anticancer and antiangiogenic drug development.
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