Novel indolocarbazole compound 6-N-formylamino-12,13-dihydro-1,11-dihydroxy- 13-(beta-D-glucopyranosyl)-5H-indolo[2,3-a]pyrrolo-[3,4-c]carbazole- 5,7(6H)-dione (NB-506): its potent antitumor activities in mice.

Abstract

NB-506 [6-N-formylamino-12,13-dihydro-1,11-dihydroxy-13-(beta-D- glucopyranosyl)-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-di one d is a new antitumor indolocarbazole compound. The growths of murine M5076 and Ehrlich solid tumors were inhibited 76 and 96%, respectively, by i.v. injection at doses of 300 mg/m2. Furthermore, NB-506 caused regression of nodules of human PC-13 lung cancer and MKN-45 stomach cancer cells at i.v. doses of 90 mg/m2. Human HCT 116 and LS 180 colon cancers also regressed with injections of NB-506. Repeated injections of NB-506 had a stronger antitumor effect than intermittent injections in mice with MKN-45. The cumulative toxicity of NB-506 was low in terms of lethality in mice, i.e., the LD50s on single and 10 repeated i.v. injections into CDF1 mice were 990 and 810 mg/m2/injection, respectively. In conclusion, NB-506 is considered to be an interesting possible candidate as an anticancer drug for treatment of solid tumors in humans.

• Authors: H Arakawa, T Iguchi, M Morita, T Yoshinari, K Kojiri, H Suda, A Okura, S Nishimura
• Journal: Cancer research (Cancer Res) Vol. 55 Issue 6 Pg. 1316-20 (Mar 15 1995) ISSN: 0008-5472 [Print] United States
• PMID: 7882329 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Carbazoles
• Glucosides
• NB 506

Topics

• Animals
• Antineoplastic Agents (therapeutic use)
• Carbazoles (pharmacology, therapeutic use)
• Female
• Glucosides (pharmacology, therapeutic use)
• Humans
• Lethal Dose 50
• Mice
• Mice, Inbred BALB C
• Neoplasms, Experimental (drug therapy)
• Tumor Cells, Cultured (drug effects)