New Invention Profile
| Publication No: | IN202411036881 [India] | Application No: | IN202411036881 |
| Title: | 2-pyridone based quinazoline compounds as dual ezh2 and EGFR inhibitors | ||
| Publication Date: | 28-11-2025 | File Date: | 09-05-2024 |
| Inventor(s): | Arpita Banerjee; Saumya Ranjan Satrusal; Indranil Chatterjee; Priyanka Rai; Muqtada Ali Khan; Arpon Biswas; Rabi Sankar Bhatta; Jiaur Rahaman Gayen; Aamir Nazir; Gautam Panda; Dipak Datta | ||
| IPC Classification: | A61K31/4545, A61K31/4433, A61K31/519, A61P35/00, C07D405/14, C07D471/04 | ||
| Abstract: | The present invention relates to a 2-Pyridone-based quinazoline compound that functions as a dual EZH2 and EGFR inhibitor, offering potential therapeutic applications in cancer treatment. It further provides a process for synthesizing these compounds. The developed compounds demonstrate superior cytotoxic activity against TNBC cells compared to individual comparator drugs, namely Tazemetostat (EZH2 inhibitor) and Gefitinib (EGFR inhibitor). Among them, S-023-0996 (41a) exhibited significant efficacy in in vitro assays. Pharmacokinetic studies revealed that S-023-0996 (41a) is a dual inhibitor with 19.81% bioavailability. Moreover, subcutaneous administration of S-023-0996 (41a) at 100 mg/kg every other day led to a notable reduction in primary tumor burden, achieving 60% tumor growth inhibition, while ex vivo imaging confirmed its effectiveness in suppressing TNBC metastasis. |
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Industrial Applications
Chemistry, Chemical Processes Polymers [Chemistry, Chemical Processes]
Synhtesis Procesess [Drugs and Pharmaceuticals]