title: 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.
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 InCl3was 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.
authors.affiliation: Department of Chemistry, Osmania University, Hyderabad 500046, India.
authors.lastname: Ismail
authors.affiliation: Department of Chemistry, Osmania University, Hyderabad 500046, India.
authors.forename: Bhaskar
authors.initials: B
authors.lastname: Kuthati
authors.affiliation: Department of Chemistry, Osmania University, Hyderabad 500046, India.
authors.forename: Gangadhar
authors.initials: G
authors.lastname: Thalari
authors.affiliation: DR Reddy's Institute of Lifesciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India.
authors.forename: Venkatesham
authors.initials: V
authors.lastname: Bommarapu
authors.affiliation: Department of Biochemistry, Sri Krishnadevaraya University, Anantapur 515001, India.
authors.forename: Chaitanya
authors.initials: C
authors.lastname: Mulakayala
authors.affiliation: Department of Biochemistry, Sri Krishnadevaraya University, Anantapur 515001, India.
authors.forename: Suresh Kumar
authors.initials: SK
authors.lastname: Chitta
authors.affiliation: DR Reddy's Institute of Lifesciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India. Electronic address: naveen071280@gmail.com.
authors.forename: Naveen
authors.initials: N
authors.lastname: Mulakayala
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D066241:Carbon-13 Magnetic Resonance Spectroscopy; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D013058:Mass Spectrometry; D066244:Proton Magnetic Resonance Spectroscopy; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011743:Pyrimidines
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