MUMBAI, India, Oct. 26 -- Intellectual Property India has published a patent application (202521079040 A) filed by Institute Of Pharmacy, Nirma University on August 20, 2025, for Novel Acridine Derivatives With Anticancer Activity And Method Of Synthesis Thereof.
Inventors include Dr. Hardik Bhatt; Mr. Rajdeep Dey; Dr. Bhumika Patel; and Dr. Vivek Vyas.
The application for the patent was published on October 23, 2026, under issue no. 43/2026.
Abstract: ABSTRACT NOVEL ACRIDINE DERIVATIVES WITH ANTICANCER ACTIVITY AND METHOD OF SYNTHESIS THEREOF The invention relates to novel acridine derivatives with potent anticancer activity and methods for their synthesis. A library of fifty seven substituted acridines was prepared in two series: Series 1, comprising N-substituted acridine 9-amine derivatives bearing a -NH–R2 linker at C-9 and R1 substituents selected from H, 2 methoxy, 2 methyl and 2 fluoro; and Series 2, comprising N-(acridin-9-yl)-amide derivatives bearing a -NH–CO–R linker at C-9. The synthetic route involves copper catalysed amidation of o- chlorobenzoic acid with substituted anilines, POCl3 mediated cyclisation to 9-chloroacridines and subsequent C-9 functionalisation by nucleophilic substitution or amide formation. Structures were confirmed by ¹H NMR, ¹³C NMR, IR, mass spectrometry and single crystal X ray analysis for representative compounds. The derivatives exhibit sub micromolar to nanomolar IC50 values against human cancer cell lines A549, HT 29, HepG2, MCF 7 and K 562 in MTT assays, with limited toxicity toward VERO cells. In particular, Compound 14 shows nanomolar potency in A549 and MCF 7 cells.
Disclaimer: Curated by HT Syndication.
