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.

• Authors: M F Braña, J M Castellano, C M Roldán, A Santos, D Vázquez, A Jiménez
• Journal: Cancer chemotherapy and pharmacology (Cancer Chemother Pharmacol) Vol. 4 Issue 1 Pg. 61-6 ( 1980) ISSN: 0344-5704 [Print] Germany
• PMID: 6153938 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Imides
• Isoquinolines
• Naphthalimides
• Neoplasm Proteins
• Nitro Compounds
• Pyrrolidines
• mitonafide
• pinafide
• RNA

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, toxicity)
• Carcinoma, Ehrlich Tumor (drug therapy)
• Cell Survival (drug effects)
• DNA Replication (drug effects)
• HeLa Cells (drug effects)
• Humans
• Imides
• Isoquinolines (administration & dosage, chemical synthesis, therapeutic use)
• Lethal Dose 50
• Mice
• Naphthalimides
• Neoplasm Proteins (biosynthesis)
• Nitro Compounds (administration & dosage, chemical synthesis, therapeutic use)
• Pyrrolidines (administration & dosage, chemical synthesis, therapeutic use)
• RNA (biosynthesis)
• Rats
• Spectrophotometry, Infrared