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Antitumor activity on murine tumors of a novel antitumor benzoylphenylurea derivative, HO-221.

Abstract
A novel antitumor compound, N-[4-(5-bromo-2-pyrimidinyloxy)-3-chlorophenyl]-N'-(2-nitrobenzoyl ) urea (HO-221) was evaluated for its antitumor activity in experimental tumor models. HO-221 preparation was given orally to tumor-bearing animals. The compound exhibited significant effects against various tumors such as P388 and L1210 leukemias; M5076 reticulum-cell sarcoma; colon 38 carcinoma; human xenografts MX-1, LX-1, GA-1, and Co-1; Lewis lung carcinoma; sarcoma 180; and Walker 256 carcinosarcoma and was especially effective against solid tumors. However, its effect on murine B16 melanoma was moderate. Intermittent administration of HO-221 produced better results. The effects of HO-221 on human tumor xenografts were compared with those of other antitumor agents. HO-221 showed activity against LX-1 lung and Co-1 gastrointestinal tumor and was also effective against advanced-stage L1210 leukemia and Lewis lung carcinoma. Furthermore, the effect of HO-221 on drug-resistant tumors was examined using murine leukemias L1210 and P388. It showed no cross-resistance with the known antitumor agents Adriamycin (ADM), daunomycin (DM), vincristine (VCR), mitomycin C (MMC), cisplatin (CDDP), 5-fluorouracil (5-FU), cytosine arabinoside (Ara-C), methotrexate (MTX), cyclophosphamide (CPA), or carboquone (CQ), and collateral sensitivity to HO-221 was found in MMC-, CDDP-, and CPA-resistant sublines. HO-221 exhibits significant reproducible, broad-spectrum antitumor activity against experimental tumors as well as human neoplasms.
AuthorsT Nakajima, H Masuda, T Okamoto, M Watanabe, K Yokoyama, N Yamada, S Fujimoto, S Tsukagoshi, T Taguchi
JournalCancer chemotherapy and pharmacology (Cancer Chemother Pharmacol) Vol. 28 Issue 5 Pg. 351-6 ( 1991) ISSN: 0344-5704 [Print] Germany
PMID1914078 (Publication Type: Journal Article)
Chemical References
  • Antineoplastic Agents
  • Benzamides
  • Nitrobenzenes
  • N-(4-(5-bromo-2-pyrimidinyloxy)-3-chlorophenyl)-N'-(2-nitrobenzoyl)urea
Topics
  • Animals
  • Antineoplastic Agents (therapeutic use)
  • Benzamides (therapeutic use)
  • Dose-Response Relationship, Drug
  • Drug Resistance
  • Drug Screening Assays, Antitumor
  • Female
  • Leukemia, Experimental (drug therapy)
  • Male
  • Mice
  • Mice, Inbred Strains
  • Neoplasm Transplantation
  • Neoplasms, Experimental
  • Nitrobenzenes (therapeutic use)
  • Rats

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