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. 1993 Jun;67(6):1293–1298. doi: 10.1038/bjc.1993.240

Anti-proliferative effects of the arotinoid Ro 40-8757 on human cancer cell lines in vitro.

J F Eliason 1, F Kaufmann 1, T Tanaka 1, T Tsukaguchi 1
PMCID: PMC1968519  PMID: 8390284

Abstract

A novel arotinoid with a morpholine structure in the polar end group Ro 40-8757 (4-[2-[p-[(E)-2(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2- naphthyl)propenyl]phenoxy]ethyl]-morpholine) was tested for its anti-proliferative activity against nine human cancer cell lines in vitro. The lines included two estrogen receptor positive breast cancer lines (MCF-7 and ZR-75-1), two estrogen receptor negative breast cancer lines (MDA-MB-231 and BT-20), one cervix carcinoma line (KB-3-1), two lung adenocarcinoma lines (A549 and HLC-1), one large cell lung cancer line (LXFL 529) and two colorectal lines (CXF 243 and CXF 280). Proliferation of all the lines, except the two lung adenocarcinoma lines, was inhibited by lower concentrations of Ro 40-8757 than those of all-trans retinoic acid (RA) or 13-cis RA giving the same level of inhibition. The degree of inhibition of RO 40-8757 was concentration and time dependent. The arotinoid was not cytotoxic and morphological signs by differentiation were not evident in cultures treated with Ro 40-8757 for up to 2 weeks. Because this compound is active on cells such as KB-3-1 that are not inhibited by all-trans RA and because it does not bind to nuclear retinoic acid receptors, it may represent a novel class of anti-proliferative agents.

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Selected References

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  1. Bollag W., Hartmann H. R. Inhibition of rat mammary carcinogenesis by an arotinoid without a polar end group (Ro 15-0778). Eur J Cancer Clin Oncol. 1987 Feb;23(2):131–135. doi: 10.1016/0277-5379(87)90006-x. [DOI] [PubMed] [Google Scholar]
  2. Castaigne S., Chomienne C., Daniel M. T., Ballerini P., Berger R., Fenaux P., Degos L. All-trans retinoic acid as a differentiation therapy for acute promyelocytic leukemia. I. Clinical results. Blood. 1990 Nov 1;76(9):1704–1709. [PubMed] [Google Scholar]
  3. Chomienne C., Ballerini P., Balitrand N., Amar M., Bernard J. F., Boivin P., Daniel M. T., Berger R., Castaigne S., Degos L. Retinoic acid therapy for promyelocytic leukaemia. Lancet. 1989 Sep 23;2(8665):746–747. doi: 10.1016/s0140-6736(89)90812-x. [DOI] [PubMed] [Google Scholar]
  4. Chomienne C., Ballerini P., Balitrand N., Daniel M. T., Fenaux P., Castaigne S., Degos L. All-trans retinoic acid in acute promyelocytic leukemias. II. In vitro studies: structure-function relationship. Blood. 1990 Nov 1;76(9):1710–1717. [PubMed] [Google Scholar]
  5. Crettaz M., Baron A., Siegenthaler G., Hunziker W. Ligand specificities of recombinant retinoic acid receptors RAR alpha and RAR beta. Biochem J. 1990 Dec 1;272(2):391–397. doi: 10.1042/bj2720391. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Eliason J. F., Aapro M. S., Decrey D., Brink-Petersen M. Non-linearity of colony formation by human tumour cells from biopsy samples. Br J Cancer. 1985 Sep;52(3):311–318. doi: 10.1038/bjc.1985.195. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Eliason J. F., Fekete A., Odartchenko N. Improving techniques for clonogenic assays. Recent Results Cancer Res. 1984;94:267–275. doi: 10.1007/978-3-642-82295-7_29. [DOI] [PubMed] [Google Scholar]
  8. Eliason J. F. Long-term production of hemopoietic progenitors in cultures containing low levels of serum. Exp Hematol. 1984 Aug;12(7):559–567. [PubMed] [Google Scholar]
  9. Eliason J. F., Ramuz H., Kaufmann F. Human multi-drug-resistant cancer cells exhibit a high degree of selectivity for stereoisomers of verapamil and quinidine. Int J Cancer. 1990 Jul 15;46(1):113–117. doi: 10.1002/ijc.2910460121. [DOI] [PubMed] [Google Scholar]
  10. Hong W. K., Lippman S. M., Itri L. M., Karp D. D., Lee J. S., Byers R. M., Schantz S. P., Kramer A. M., Lotan R., Peters L. J. Prevention of second primary tumors with isotretinoin in squamous-cell carcinoma of the head and neck. N Engl J Med. 1990 Sep 20;323(12):795–801. doi: 10.1056/NEJM199009203231205. [DOI] [PubMed] [Google Scholar]
  11. Huang M. E., Ye Y. C., Chen S. R., Chai J. R., Lu J. X., Zhoa L., Gu L. J., Wang Z. Y. Use of all-trans retinoic acid in the treatment of acute promyelocytic leukemia. Blood. 1988 Aug;72(2):567–572. [PubMed] [Google Scholar]
  12. Lippman S. M., Kavanagh J. J., Paredes-Espinoza M., Delgadillo-Madrueño F., Paredes-Casillas P., Hong W. K., Holdener E., Krakoff I. H. 13-cis-retinoic acid plus interferon alpha-2a: highly active systemic therapy for squamous cell carcinoma of the cervix. J Natl Cancer Inst. 1992 Feb 19;84(4):241–245. doi: 10.1093/jnci/84.4.241. [DOI] [PubMed] [Google Scholar]
  13. Lippman S. M., Kessler J. F., Meyskens F. L., Jr Retinoids as preventive and therapeutic anticancer agents (Part I). Cancer Treat Rep. 1987 Apr;71(4):391–405. [PubMed] [Google Scholar]
  14. Lippman S. M., Kessler J. F., Meyskens F. L., Jr Retinoids as preventive and therapeutic anticancer agents (Part II). Cancer Treat Rep. 1987 May;71(5):493–515. [PubMed] [Google Scholar]
  15. Lippman S. M., Parkinson D. R., Itri L. M., Weber R. S., Schantz S. P., Ota D. M., Schusterman M. A., Krakoff I. H., Gutterman J. U., Hong W. K. 13-cis-retinoic acid and interferon alpha-2a: effective combination therapy for advanced squamous cell carcinoma of the skin. J Natl Cancer Inst. 1992 Feb 19;84(4):235–241. doi: 10.1093/jnci/84.4.235. [DOI] [PubMed] [Google Scholar]
  16. Plumb J. A., Milroy R., Kaye S. B. Effects of the pH dependence of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide-formazan absorption on chemosensitivity determined by a novel tetrazolium-based assay. Cancer Res. 1989 Aug 15;49(16):4435–4440. [PubMed] [Google Scholar]
  17. Teelmann K., Bollag W. Therapeutic effect of the arotinoid Ro 15-0778 on chemically induced rat mammary carcinoma. Eur J Cancer Clin Oncol. 1988 Jul;24(7):1205–1209. doi: 10.1016/0277-5379(88)90129-0. [DOI] [PubMed] [Google Scholar]
  18. Warrell R. P., Jr, Frankel S. R., Miller W. H., Jr, Scheinberg D. A., Itri L. M., Hittelman W. N., Vyas R., Andreeff M., Tafuri A., Jakubowski A. Differentiation therapy of acute promyelocytic leukemia with tretinoin (all-trans-retinoic acid). N Engl J Med. 1991 May 16;324(20):1385–1393. doi: 10.1056/NEJM199105163242002. [DOI] [PubMed] [Google Scholar]

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