AI Article Synopsis
- Cysteine-dependent caspase activation plays a key role in apoptosis, and inhibiting caspase-3 may help reduce cell damage following a stroke.
- Researchers have identified a new class of compounds, 3,4-dihydropyrimido(1,2-a)indol-10(2H)-ones, as potential small molecule inhibitors of caspase-3.
- The study covers the synthesis, biological testing, and the relationship between the structure and activity of these pyrimidoindolone compounds.
Article Abstract
Cysteine-dependant aspartyl protease (caspase) activation has been implicated as a part of the signal transduction pathway leading to apoptosis. It has been postulated that caspase-3 inhibition could attenuate cell damage after an ischemic event and thereby providing for a novel neuroprotective treatment for stroke. As part of a program to develop a small molecule inhibitor of caspase-3, a novel series of 3,4-dihydropyrimido(1,2-a)indol-10(2H)-ones (pyrimidoindolones) was identified. The synthesis, biological evaluation and structure-activity relationships of the pyrimidoindolones are described.
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| http://dx.doi.org/10.1016/j.bmc.2009.09.036 | DOI Listing |
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