Amonafide Research Paper

Naphthalimide derivatives are classified under intercalators, having a flat aromatic or heteroaromatic moiety and basic side chains. Amonafide is one of the most widely studied naphthalimides, which binds DNA by intercalation and also as Topoisomerase II inhibitors. The napthalimides showed excellent activity in breast cancer trials but failed in phase III trials due to its side effects and bone marrow toxicity [54]. The justly Naphtalene diimide (NDI) scaffold achieved recently as intercalators and enhance, stabilize, alkylate G-quadruplex are major breakthrough [52]. Restricted analogues of isoCA-4 were designed and a novel series of dihydronaphtalene, tetrahydronaphtalene and naphtalene derivatives were synthesized and cytotoxicity studies
In the same year Pradidphol synthesized novel naphthoquinone aromatic amides and evaluated for anticancer activity. Benzamide 80 showed potent inhibition against NCI-H187 cell lines while naphthamides 81 and 83 were the most potent inhibition against KB cells. The decatenation assay revealed that compounds 82 and 83 inhibit hTopoIIa activity at 20 µM, while three other compounds 81, 82, and 84, exhibited hTopoIIα inhibitory activity at concentration of 50 µM [53]. Novel oxo-heterocyclic fused naphthalimide derivatives were prepared and showed potent antiproliferative activity along with their thio-heterocyclic fused analogs by Tan et al., 2013. Further studies showed that compounds 85, 86 and 87, 88 showed strong inhibition activity both to topo II & topo I [54]. Chen et al., 2013 synthesized N-(naphthalen-2-yl)acetamide and N-(substituted phenyl)acetamide bearing quinolin-2(1H)-one and 3,4-dihydroquinolin-2(1H)-one derivatives and in vitro antiproliferative activities against a panel of human cancer cell lines including nasopharyngeal (NPCTW01), lung carcinoma (H661), hepatoma (Hep3B), renal carcinoma (A498), and gastric cancer (MKN45) was done. Compound 89