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Keywords = indenopyrazole

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8 pages, 2368 KiB  
Communication
Synthesis and Characterization of 3-Methyl-1-(4-(trifluoromethyl)phenyl)indeno [1,2-c]pyrazol-4(1H)-one
by Linh Lam, Sang H. Park and Joseph Sloop
Molbank 2022, 2022(4), M1483; https://doi.org/10.3390/M1483 - 7 Nov 2022
Viewed by 3138
Abstract
Pyrazoles have potential applications in the agrochemical and medicinal chemistry industries as pesticides, anti-inflammatory medications, and antitumor drugs. Fluorinated fused-ring pyrazoles may also possess medicinally useful properties. Herein, we report the acid-catalyzed synthesis of a new tricyclic, trifluoromethylated indenopyrazole, 3-methyl-1-(4-(trifluoromethyl)phenyl)indeno[1,2-c]pyrazol-4(1H)-one, from [...] Read more.
Pyrazoles have potential applications in the agrochemical and medicinal chemistry industries as pesticides, anti-inflammatory medications, and antitumor drugs. Fluorinated fused-ring pyrazoles may also possess medicinally useful properties. Herein, we report the acid-catalyzed synthesis of a new tricyclic, trifluoromethylated indenopyrazole, 3-methyl-1-(4-(trifluoromethyl)phenyl)indeno[1,2-c]pyrazol-4(1H)-one, from 2-acetyl-1,3-indanedione and 4-trifluoromethylphenylhydrazine. This isomeric pyrazole was obtained in yields ranging from 4–24%. NMR spectroscopic characterization and elemental analysis support the structural assignment, identity, and purity of the product. Full article
(This article belongs to the Collection Heterocycle Reactions)
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15 pages, 2078 KiB  
Article
A New Series of Indeno[1,2-c]pyrazoles as EGFR TK Inhibitors for NSCLC Therapy
by Ahmet Özdemir, Halilibrahim Ciftci, Belgin Sever, Hiroshi Tateishi, Masami Otsuka, Mikako Fujita and Mehlika Dilek Altıntop
Molecules 2022, 27(2), 485; https://doi.org/10.3390/molecules27020485 - 13 Jan 2022
Cited by 6 | Viewed by 2552
Abstract
Non-small cell lung cancer (NSCLC) is the leading cause of cancer-related death throughout the world. Due to the shortcomings of traditional chemotherapy, targeted therapies have come into prominence for the management of NSCLC. In particular, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor [...] Read more.
Non-small cell lung cancer (NSCLC) is the leading cause of cancer-related death throughout the world. Due to the shortcomings of traditional chemotherapy, targeted therapies have come into prominence for the management of NSCLC. In particular, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) therapy has emerged as a first-line therapy for NSCLC patients with EGFR-activating mutations. In this context, new indenopyrazoles, which were prepared by an efficient microwave-assisted method, were subjected to in silico and in vitro assays to evaluate their potency as EGFR TK-targeted anti-NSCLC agents. Compound 4 was the most promising antitumor agent towards A549 human lung adenocarcinoma cells, with an IC50 value of 6.13 µM compared to erlotinib (IC50 = 19.67 µM). Based on its low cytotoxicity to peripheral blood mononuclear cells (PBMCs), it can be concluded that compound 4 exerts selective antitumor action. This compound also inhibited EGFR TK with an IC50 value of 17.58 µM compared to erlotinib (IC50 = 0.04 µM) and induced apoptosis (56.30%). Taking into account in silico and in vitro data, compound 4 stands out as a potential EGFR TKI for the treatment of NSCLC. Full article
(This article belongs to the Special Issue Targeted Anticancer Drug Discovery)
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