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Triphenyltin(IV) acylhydrazone compounds: Synthesis, structure and bioactivity
Xicheng Liu1, Yanhua Tang1, Xiangdong He1
1Institute of Anticancer Agents Development and Theranostic Application, The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine, School of Chemistry and Chemical Engineering, Qufu Normal University, Qufu 273165, China.
Four novel triphenyltin(IV) compounds were synthesized and exhibit potent anticancer activity against lung cancer cells. These compounds show promise by effectively inducing apoptosis and generating reactive oxygen species.
Area of Science:
- Organometallic Chemistry
- Medicinal Chemistry
- Biochemistry
Background:
- Triphenyltin(IV) compounds are explored for their biological activities.
- Acylhydrazone derivatives offer diverse chemical properties.
- Understanding structure-activity relationships is crucial for drug development.
Purpose of the Study:
- To synthesize and characterize novel triphenyltin(IV) acylhydrazone compounds.
- To investigate the binding properties of these compounds with bovine serum albumin (BSA).
- To evaluate the cytotoxic activity of the synthesized compounds against human lung cancer cells.
Main Methods:
- Synthesis of four triphenyltin(IV) acylhydrazone compounds.
- Characterization using elemental analysis, IR, NMR, and MS.
- Crystal structure determination.
- In vitro bioassays to assess cytotoxicity and mechanism of action.
Main Results:
- Successful synthesis and characterization of four new triphenyltin(IV) acylhydrazone compounds.
- Crystal structures revealed four-coordinated tin atoms with pseudo-tetrahedral geometry.
- Compounds demonstrated strong binding to BSA and oxidized NADH, generating reactive oxygen species (ROS).
- The compounds exhibited superior cytotoxic activity against A549 lung cancer cells compared to cisplatin, with notable selectivity.
Conclusions:
- The synthesized triphenyltin(IV) acylhydrazone compounds possess significant cytotoxic potential against lung cancer.
- Their mechanism involves ROS generation and induction of apoptosis.
- These compounds represent promising candidates for further development as anticancer agents.
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