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Chemical Compound Review:

Ethazolastone 3-ethyl-2-oxo-1,3,4,5,8...

Synonyms: CHEMBL38014, SureCN13027962, Ccrg 82019, NSC-652944, AC1L2QXL, ...

Bull, V.L. et al., Tisdale, M.J., Zucchetti, M. et al., Tisdale, M.J.

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Disease relevance of NSC652944

In contrast neither chlorambucil or the ethylimidazotetrazinone (CCRG 82019) showed differential toxicity between Mer+ and Mer- cell lines [1].

High impact information on NSC652944

Ethazolastone (its 3-ethylimidazo analogue) which does not cause differentiation of K562 produced no significant DNA damage and G2 phase blockade [2].
The extent of macromolecular alkylation by three imidazotetrazinones, 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4-(3H )-one (mitozolomide) and the 3-methyl CCRG 81045) and 3-ethyl (CCRG 82019) analogues has been studied both in intact cells and with isolated DNA, RNA and protein [3].
Calf thymus DNA modified with CCRG 82019 was more effective as a methylase inhibitor than DNA modified with Temozolomide, which was a reverse of the order of potencies of the free drugs against tumour cells in culture [4].

References

Antitumor imidazotetrazines--XV. Role of guanine O6 alkylation in the mechanism of cytotoxicity of imidazotetrazinones. Tisdale, M.J. Biochem. Pharmacol. (1987) [Pubmed]
Temozolomide induced differentiation of K562 leukemia cells is not mediated by gene hypomethylation. Zucchetti, M., Catapano, C.V., Filippeschi, S., Erba, E., D'Incalci, M. Biochem. Pharmacol. (1989) [Pubmed]
Antitumour imidazotetrazines--XVI. Macromolecular alkylation by 3-substituted imidazotetrazinones. Bull, V.L., Tisdale, M.J. Biochem. Pharmacol. (1987) [Pubmed]
Antitumour imidazotetrazines and gene expression. Tisdale, M.J. Acta oncologica (Stockholm, Sweden) (1988) [Pubmed]

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