Literature DB >> 28216402

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.

Bhaskar Kuthati1, Gangadhar Thalari1, Venkatesham Bommarapu2, Chaitanya Mulakayala3, Suresh Kumar Chitta3, Naveen Mulakayala4.   

Abstract

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-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.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

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

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Substances:

Year:  2017        PMID: 28216402     DOI: 10.1016/j.bmcl.2017.01.088

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

Review 1.  Spirocyclic derivatives as antioxidants: a review.

Authors:  Karen Acosta-Quiroga; Cristian Rojas-Peña; Luz Stella Nerio; Margarita Gutiérrez; Efraín Polo-Cuadrado
Journal:  RSC Adv       Date:  2021-06-21       Impact factor: 4.036

Review 2.  Herbal Compounds Play a Role in Neuroprotection through the Inhibition of Microglial Activation.

Authors:  Yan Fu; Jianmei Yang; Xingyu Wang; Pin Yang; Yang Zhao; Kun Li; Yongjun Chen; Ying Xu
Journal:  J Immunol Res       Date:  2018-04-17       Impact factor: 4.818

3.  Synthesis, Biological Evaluation and Molecular Docking Study of 2-Substituted-4,6-Diarylpyrimidines as α-Glucosidase Inhibitors.

Authors:  Zipeng Gong; Zhenzhen Xie; Jie Qiu; Guangcheng Wang
Journal:  Molecules       Date:  2017-10-30       Impact factor: 4.411

4.  Sirtuin 1 Inhibiting Thiocyanates (S1th)-A New Class of Isotype Selective Inhibitors of NAD+ Dependent Lysine Deacetylases.

Authors:  Nathalie Wössner; Zayan Alhalabi; Jessica González; Sören Swyter; Jin Gan; Karin Schmidtkunz; Lin Zhang; Alejandro Vaquero; Huib Ovaa; Oliver Einsle; Wolfgang Sippl; Manfred Jung
Journal:  Front Oncol       Date:  2020-04-30       Impact factor: 6.244

  4 in total

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