Naphthalimide derivatives with therapeutic characteristics: a patent review

Abstract

Introduction: Naphthalimides are important aromatic heterocycles with immense pharmacological significance as they serve as core scaffold for many antitumor, anti-inflammatory, antidepressant, antiprotozoal and antiviral agents, etc. The tricyclic planar ring system of naphthalimide is primarily responsible for its intercalation with DNA to perturb the cellular events and the substitution pattern of the molecule leads to several other applications. The promising pharmacological activity profile and ease of synthesis have been attractive in design and development of new class of naphthalimides and their conjugates as various potential therapeutic agents. Few of such molecules are currently under preclinical and clinical evaluations.

Areas covered: Important patents focusing on naphthalimides as potential class of therapeutics, published between the period of 2006 – 2011have been covered. The reports are presented together with a review of the related structural chemical space. This review mainly focuses on the therapeutic applications, structural modifications of naphthalimide scaffold, their conjugates and heterocyclics bearing naphthalimide moiety.

Expert opinion: The tricyclic planar ring system of naphthalimide restrains important pharmaceutical properties along with excellent fluorescent after proper substitution pattern. Linking these active naphthalimide derivatives with other active pharmacophore has become an interesting area of research. The utility of naphthalimide derivatives as novel pharmaceutical and photochemical agents can be further enhanced by introducing polar side chains and fusing functionalized heterocyclic rings with naphthalimide cores.

Keywords::

• antitumor activity
• DNA intercalation
• histone deacetylase inhibitor
• heterocyclic conjugates
• naphthalimides
• PARP inhibitor
• topoisomerase I inhibition