Synthesis and biological evaluation of alkali metal salts of tryptanthrin-6-oxime
| Parent link: | 53rd International Union of Pure & Applied Chemistry General Assembly (IUPAC 2025) and 50th World Chemistry Congress (50WCC).— 2025.— P. 210 |
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| Other Authors: | , |
| Summary: | Title screen Indolo[2,1-b]quinazolin-6,12-dione oxime (tryptanthrin-6-oxime, Tryp-Ox) exhibit a variety of chemical properties and pharmacological activities. Owing to ion-chelating properties, oximes can be ligands in various complexes formed by metal ions. As the complex formation can affect biological activity of oximes, we decided to obtain a series of alkali metal salts (oximates) containing the Tryp-Ox scaffold (Figure 1) and study their solubility and cytotoxicity. Previously we synthesized lithium and sodium salts of Tryp-Ox and established their high affinity for JNK1-3 (Kd < 1 μM) and potent inhibition of LPS-induced nuclear NF-κB/AP-1 activation and IL-6 production in human monocytic cells [1]. The c-Jun N-terminal kinase (JNK) pathway is a dual-functional oncogenic signaling that exerts both anti- and pro-tumor activities [2,3]. In this research we focused on evaluation the antitumor activity of oximates Текстовый файл |
| Language: | English |
| Published: |
2025
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| Subjects: | |
| Online Access: | https://iupac-2025.s3.ap-southeast-1.amazonaws.com/j3y8n5cpauaosv9ekold8novsqtj#page=210 |
| Format: | Electronic Book Chapter |
| KOHA link: | https://koha.lib.tpu.ru/cgi-bin/koha/opac-detail.pl?biblionumber=682288 |
| Summary: | Title screen Indolo[2,1-b]quinazolin-6,12-dione oxime (tryptanthrin-6-oxime, Tryp-Ox) exhibit a variety of chemical properties and pharmacological activities. Owing to ion-chelating properties, oximes can be ligands in various complexes formed by metal ions. As the complex formation can affect biological activity of oximes, we decided to obtain a series of alkali metal salts (oximates) containing the Tryp-Ox scaffold (Figure 1) and study their solubility and cytotoxicity. Previously we synthesized lithium and sodium salts of Tryp-Ox and established their high affinity for JNK1-3 (Kd < 1 μM) and potent inhibition of LPS-induced nuclear NF-κB/AP-1 activation and IL-6 production in human monocytic cells [1]. The c-Jun N-terminal kinase (JNK) pathway is a dual-functional oncogenic signaling that exerts both anti- and pro-tumor activities [2,3]. In this research we focused on evaluation the antitumor activity of oximates Текстовый файл |
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