New Invention Profile
| Publication No: | IN202411019816 [India] | Application No: | IN202411019816 |
| Title: | Amino acid and triazine based new poly(ADP-RIBOSE)polymerase (PARP) inhibitors and their application against BRCA mutated cancers | ||
| Publication Date: | 26-09-2025 | File Date: | 15-03-2024 |
| Inventor(s): | Panda, Gautam; Satrusal, Saumya Ranjan; Chatterjee, Indranil; Barman, Souvik; Ali, Kasim; Kumar, Sachin; Sinha, Supriya; Meena, Sanjeev; Gayen, Jiaur Rahaman; Nazir, Aamir; Bhadauria, Smrati; Datta, Dipak | ||
| IPC Classification: | A61P003500, A61P002500, A61P000910, A61P002528, A61P004300 | ||
| Abstract: | The invention relates to chiral amino acids as well as symmetrical diamino triazine substituted phthalazinones as Poly(ADP-ribose)polymerase (PARP) Inhibitors, process for the preparation and uses thereof as potential anticancer agents. The invention particularly relates to a process for the preparation of symmetrical for new. The compounds inhibited the growth and development of BRCA2 mutant cells with an IC50 value of the most active compounds in the range of 2-57 nM. The active compounds selectively induce cytotoxicity in BRCA2 mutant cancer cells compared to wild type cells with a mutant fold selectivity in range of 112- 2500-fold. The active compounds are capable of killing the BRCA mutated cancerous cells and show significant PARP activity as well as show low cytotoxicity to wild type cells. Most importantly, our hit molecules demonstrated approximately 50% or greater cell viability of mice HSPCs. This suggests an improved hematological safety profile of our hits, distinguishing them from FDA-approved PARP inhibitor Olaparib. |
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: director[at]cdri[dot]res[dot]in
:91-522-2772450
:https://www.cdri.res.in