Kuthati Bhaskar, Thalari Gangadhar, Bommarapu Venkatesham, Mulakayala Chaitanya, Chitta Suresh Kumar, Mulakayala Naveen
Department of Chemistry, Osmania University, Hyderabad 500046, India.
DR Reddy's Institute of Lifesciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India.
Bioorg Med Chem Lett. 2017 Mar 15;27(6):1446-1450. doi: 10.1016/j.bmcl.2017.01.088. Epub 2017 Feb 1.
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 InCl was reported. This method has been extended for the synthesis of novel spiro[benzo[4,5]thieno[2,3-d]pyrimidine-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.
报道了一种高效新颖的方法，即在温和条件下使用催化量的三氯化铟，通过4-氨基-1-甲基-3-丙基吡唑-5-甲酰胺与酮缩合制备螺[吡唑并[4,3-d]嘧啶]-7'(1'H)-酮。该方法已扩展用于合成新型螺[苯并[4,5]噻吩并[2,3-d]嘧啶-2,3'-吲哚啉]-2',4(3H)-二酮，这些化合物在药物化学中具有潜在应用。对所有合成化合物进行了体外抗增殖活性评估，发现几种化合物具有活性。进一步的体外研究表明，抑制沉默调节蛋白可能是这些分子的作用机制。
