Benzothiazine based acetohydrazides and acetamides as anticancer agents.
Sana Aslam1, Fang Wang2, Matloob Ahmad3
1Department of Chemistry, Government College Women University, Faisalabad, Pakistan.
Pakistan Journal of Pharmaceutical Sciences
|February 7, 2020
Summary
New pyrazolobenzothiazine derivatives show potent anticancer activity. Six compounds were more effective than 5-fluorouracil against oral cancer cells, with some exhibiting selective toxicity.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Oncology
Background:
- Cancer remains a leading cause of mortality worldwide, necessitating the development of novel therapeutic agents.
- Pyrazolobenzothiazine scaffolds represent a promising class of heterocyclic compounds with potential biological activities.
Purpose of the Study:
- To synthesize and evaluate the anticancer potential of novel pyrazolobenzothiazine derivatives.
- To identify compounds with selective activity against various human cancer cell lines.
Main Methods:
- Four series of pyrazolobenzothiazine derivatives were synthesized.
- Anticancer activity was assessed using the MTT assay against six human cancer cell lines: KB, MCF-7, A549, Hep-G2, SGC-7901, and S1.
- Cytotoxicity was evaluated against human peripheral blood mononuclear (PBM) cells.
Main Results:
- Six compounds (1a, 1b, 1d, 4a, 4d, 4e) demonstrated superior activity compared to 5-fluorouracil against the KB (human oral carcinoma) cell line.
- Compounds 2b and 2c exhibited activity comparable to 5-fluorouracil against the KB cell line.
- Eight compounds displayed selective anticancer activity, showing no toxicity to human PBM cells.
Conclusions:
- Pyrazolobenzothiazine derivatives hold significant promise as anticancer agents.
- Specific derivatives show potent and selective activity against oral carcinoma cells, warranting further investigation for therapeutic development.
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