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The antitumor activity and the structure of bis(adeninato-N9) diphenyltin(IV)
R Barbieri1, G Ruisi, G Atassi
1Dipartimento di Chimica Inorganica, Università di Palermo, Italy.
Abstract:
Bis(adeninato-N9)diphenyltin(IV) has been selected as a tumor panel compound by the U.S. National Cancer Institute and tested against a number of tumors according to standard protocols. The activity criteria were not passed. The solid state structure of the environment of tin in the complex has been definitely established to be of the tetrahedral type by means of 119Sn Mössbauer-Zeeman spectroscopy; this configuration has been assumed to be maintained also in aqueous suspensions of the drug, in conditions corresponding to the administration to mice. The occurrence of strong Sn-N bonds, consistently resistant to hydrolytic processes, has been assumed, and correlated to the observed low toxicity of the drug. The extent of the antitumor action corresponds to the standard response to Ph2SnIV moieties.
Insights
Bis(adeninato-N9)diphenyltin(IV) showed low antitumor activity in National Cancer Institute tumor panel tests. Its tetrahedral tin structure and strong Sn-N bonds contribute to low toxicity, aligning with diphenyltin(IV) compound responses.
Area of Science:
- Organometallic Chemistry
- Medicinal Chemistry
- Materials Science
Background:
- Bis(adeninato-N9)diphenyltin(IV) was evaluated as a potential anticancer agent.
- The U.S. National Cancer Institute included it in their tumor panel screening.
- Standard protocols were employed for efficacy assessment.
Purpose of the Study:
- To determine the antitumor activity of Bis(adeninato-N9)diphenyltin(IV).
- To elucidate the structural and bonding characteristics of the tin complex.
- To correlate structural features with observed toxicity and activity.
Main Methods:
- Tumor panel testing against various cancer models.
- 119Sn Mössbauer-Zeeman spectroscopy for solid-state structure determination.
- Assessment of hydrolytic stability and assumed in vivo behavior.
Main Results:
- The compound did not meet the activity criteria for the tumor panel.
- Solid-state 119Sn Mössbauer-Zeeman spectroscopy confirmed a tetrahedral environment around tin.
- Strong tin-nitrogen bonds were inferred, suggesting resistance to hydrolysis.
- Low toxicity was observed and correlated with the compound's structural stability.
- Antitumor action was consistent with other diphenyltin(IV) compounds.
Conclusions:
- Bis(adeninato-N9)diphenyltin(IV) exhibits limited antitumor efficacy.
- The tetrahedral tin coordination and robust Sn-N bonds contribute to its low toxicity profile.
- Structural stability is a key factor in the pharmacological behavior of this organotin compound.