Full Length Article6-(2-Morpholinoethyl)-thiazolo[3,2-a]pyrimidin-5-one: A novel scaffold for the synthesis of potential PI3kα inhibitors

Add time:09/25/2019    Source:sciencedirect.com

The present study involves the development of certain thiazolo[3,2-a]pyrimidin-5-ones linked through an ethylene bridge to various amines. The newly synthesized compounds 4–6(a–c) were subjected to in vitro anticancer evaluation using NCI antitumor screening. The target compounds showed observed activity against Renal UO-31 cancer cell line with cell growth promotion 52.72–64.52%. COMPARE analyses revealed compounds 4a and 4b exhibiting high correlation levels with rapamycin (mTOR inhibitor). Kinase assays were performed for compounds 4a and 4b on mTOR and structurally-related PI3Kα. They displayed moderate activity against PI3Kα with IC50 values of 120 and 151 μM, respectively. Compounds 4a and 4b could thus be considered as a promising leading scaffold for further development of potential PI3Kα inhibitors.

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