4.5 Article

Synthesis of novel spiro[pyrazolo[4,3-d]pyrimidinones and spiro[benzo[4,5]thieno[2,3-d]pyrimidine-2,3′-indoline]-2′,4(3H)-diones and their evaluation for anticancer activity

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 6, 页码 1446-1450

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.01.088

关键词

Spiro[pyrazolo[4,3-d]pyrimidin]-7 '(I ' H)-ones; 4-Amino-1-methyl-3-propylpyrazole-5-carboxamide; Spiro[benzo[4,5]thieno[2,3-d]pyrimidine-2,3 '-indoline]-2 ',4(3H)-dione; InCl3; Anticancer agents

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An efficient and novel method for the preparation of spiro[pyrazolo[4,3-d]pyrimidin]-7'(1'H)-ones by the condensation of 4-amino-1-methyl-3-propylpyrazole-5-carboxamide with ketones under mild conditions using catalytic InCl3 was reported. This method has been extended for the synthesis of novel spiro[benzo[4,5]thieno[2,3-dlpyrimidine-2,3'-indoline]-2',4(3H)-dione which are having potential applications in medicinal chemistry. All the synthesized compounds were evaluated for their anti-proliferative properties in vitro against cancer cell lines and several compounds were found to be active. Further in vitro studies revealed that inhibition of sirtuins could be the possible mechanism of action of these molecules. (C) 2017 Elsevier Ltd. All rights reserved.

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