Synthesis and mode(s) of action of a new series of imide derivatives of 3-nitro-1,8 naphthalic acid

Abstract

Four new imide derivatives of 3-nitro-1,8-naphthalic acid have been synthesised. The compounds show strong cytostatic activity against both HeLa and KB cells and are moderately toxic towards both mice and rats (LD50 above 4 mg/kg IP). Two of the most active compounds, M-4212 and M-12210, prevented the development of mouse Ehrlich ascites and rat Yoshida carcinoma. All these drugs block cell growth by inhibiting the synthesis of both DNA and RNA. In particular, both M-4212 and M-12210 raise the melting point of double-stranded DNA.

Synthesis and Photophysical Characterizations of Thermal -Stable Naphthalene Benzimidazoles

“…1,8-Naphthalimide and bisnaphthalimide derivatives are promising anticancer agents [9,10], the sulfonated derivatives are good antiviral agents with selective in vitro activity against the human immunity deficiency virus, HIV-1 [11]. Due to their photo-physical and photo-chemical properties the 1,8-naphthalimide derivatives can be used as fluorescence dyes for solar energy collectors and photosynthesis under concentrated sunlight [12], fluorescent markers in biological cells [13] as well as laser active media [14][15][16].…”

In vitro activity of amonafide against primary human tumors compared with the activity of standard agents

“…In continuing phase I studies of amonafide reported recently [4,5], amonafide at a dosage up to 260 mg/m2/day • 5 days resulted in no significant myelosuppression, its peak plasma level being 6 /zg/ml [5]. The drug's mechanism of action is believed to be DNA intercalation [6], and it does not require in vivo activation to exert the antitumor effect [1,7]. Amonafide will soon be investigated further in phase II studies in the United States.…”

“…Benzisoquinolinedione, 5-amino-2 [2-(dimethylamino) ethyl]-1H-benz [de]isoquinoline-1,3(2H)-dione (amonafide, previously named nafidamide) is one of a series of benz[de]-isoquinoline-l,3-dione compounds recently demonstrated to possess antitumor and antiviral activities [1][2][3]. Amonafide was found by the National Cancer Institute (NCI) to be active against P388 and L1210 leukemia, as well as B16 melanoma and M5076 sarcoma.…”

Thermally triggered theranostics for pancreatic cancer therapy

“…1B). Brana et al reported bisnaphthalimides as potent chemotherapeutic agents [26][27][28][29]. Bisnaphthalimide derivatives are identified to possess significant anti-tumour activity in both murine and human cancerous cells [26][27][28][29].…”