Drug intelligence / Profile preview

ethyldeshydroxy-sparsomycin

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

**Ethyldeshydroxy-sparsomycin** is a synthetic derivative of sparsomycin, a ribosomal protein synthesis inhibitor. It inhibits protein synthesis by interfering with the ribosomal peptidyl transferase center, similar to its parent compound sparsomycin. Ethyldeshydroxy-sparsomycin demonstrates antitumor activity, most notably by synergistically enhancing the efficacy of cisplatin against certain forms of leukemia such as L1210. Mechanistically, it appears to modulate the cellular detoxification response by depleting glutathione and decreasing glutathione S-transferase (GST) activity, thus potentially sensitizing tumor cells to cisplatin. Its major use and investigations have been in preclinical settings as an antineoplastic agent[1][2].

Other names
(E)-N-[1-(ethylsulfanylmethylsulfinyl)propan-2-yl]-3-(6-methyl-2,4-dioxo-1H-pyrimidin-5-yl)prop-2-enamide119410-38-7
02

Targets

PTC (50S ribosomal peptidyl transferase center)

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