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Chemical Compound Review

Tallimustine     4-[[4-[[4-[bis(2- chloroethyl)amino]phenyl]...

Synonyms: CHEMBL89705, SureCN62279, FCE-24517, DNC001408, Fce 24517, ...
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Disease relevance of Tallimustine


High impact information on Tallimustine


Chemical compound and disease context of Tallimustine

  • The screening of other distamycin derivatives, which maintain antitumour activity and exhibit much lower toxicity against human bone marrow cells than tallimustine led to the identification of brostallicin (PNU-166196) which is currently under early clinical investigation [7].

Biological context of Tallimustine

  • In contrast, the S-phase cells treated with tallimustine were not perturbed during the DNA-synthesis phase progression, and were blocked in G2 only after they had passed through the G1/S transition of a new cell cycle [8].
  • In cells which were in G1 or G2/M phases during drug treatment, tallimustine and L-PAM caused similar accumulation in G2 [8].
  • Despite the high specificity at the nucleotide level, tallimustine did not differentiate among bulk DNA and three discrete AT-rich regions of genomic DNA examined by quantitative PCR stop assay with lesion frequencies ranging from 0.23 to 0.39 lesions/kbp at 25 microM drug [9].
  • However, the 5'-TTTTGPu-3' motifs targeted by tallimustine are relatively infrequent and scattered throughout the genome [9].
  • For melphalan, tallimustine and carzelesin, the concentration inhibiting the growth of 70% of progenitor cells in vitro (ID70) was similar to the concentrations found in the serum of patients treated at the maximum tolerated dose (MTD) [10].

Anatomical context of Tallimustine


Associations of Tallimustine with other chemical compounds


Gene context of Tallimustine

  • We report that the sensitivities of MLH1-deficient and -proficient HCT116 human colon carcinoma cells were comparable after treatment with brostallicin, while tallimustine resulted in a three times lower cytotoxicity in MLH1-deficient than in -proficient cells [13].
  • MSH2-deficient HEC59 parental endometrial adenocarcinoma cells were as sensitive as the proficient HEC59+ch2 cells after brostallicin treatment, but were 1.8-fold resistant after tallimustine treatment as compared to the MSH2-proficient HEC59+ch2 counterpart [13].
  • These data indicate that the effects of Tallimustine on cell cycle progression in yeast are mediated by the RAD9 gene product [18].
  • The results obtained showed that PNU 151807 seems to have a mechanism of action completely different from that of its parent compound tallimustine, possibly involving the inhibition of cyclin-dependent kinases activity, and clearly indicate PNU 151807 as a new non-covalent minor groove binder with cytotoxic activity against cancer cells [19].
  • Accumulation of gamma-globin mRNA and induction of erythroid differentiation after treatment of human leukaemic K562 cells with tallimustine [14].

Analytical, diagnostic and therapeutic context of Tallimustine

  • Tallimustine is inactive in patients with previously treated small cell lung cancer. A phase II trial of the National Cancer Institute of Canada Clinical Trials Group [20].
  • A sensitive and reproducible HPLC method for the determination of tallimustine (I) in human plasma has been developed and validated [21].
  • Determination of tallimustine in human plasma by high-performance liquid chromatography [21].
  • The CC-1065 derivatives, Adozelesin and its prodrug, Carzelesin, and Tallimustine were found to be very effective against several murine tumours and human xenografts, and were shown to be active against experimental tumours that were resistant to other antineoplastic agents, including conventional alkylating agents [22].


  1. A phase I and pharmacokinetic study of tallimustine [PNU 152241 (FCE 24517)] in patients with advanced cancer. Weiss, G.R., Poggesi, I., Rocchetti, M., DeMaria, D., Mooneyham, T., Reilly, D., Vitek, L.V., Whaley, F., Patricia, E., Von Hoff, D.D., O'Dwyer, P. Clin. Cancer Res. (1998) [Pubmed]
  2. Tallimustine, an effective antileukemic agent in a severe combined immunodeficient mouse model of adult myelogenous leukemia, induces remissions in a phase I study. Beran, M., Jeha, S., O'Brien, S., Estey, E., Vitek, L., Zurlo, M.G., Rios, M.B., Keating, M., Kantarjian, H. Clin. Cancer Res. (1997) [Pubmed]
  3. Tallimustine in advanced previously untreated colorectal cancer, a phase II study. Punt, C.J., Humblet, Y., Roca, E., Dirix, L.Y., Wainstein, R., Polli, A., Corradino, I. Br. J. Cancer (1996) [Pubmed]
  4. Distamycin A and tallimustine inhibit TBP binding and basal in vitro transcription. Bellorini, M., Moncollin, V., D'Incalci, M., Mongelli, N., Mantovani, R. Nucleic Acids Res. (1995) [Pubmed]
  5. CCAAT-box binding protein NF-Y (CBF, CP1) recognizes the minor groove and distorts DNA. Ronchi, A., Bellorini, M., Mongelli, N., Mantovani, R. Nucleic Acids Res. (1995) [Pubmed]
  6. Combinatorial identification of a novel consensus sequence for the covalent DNA-binding polyamide tallimustine. Sunavala-Dossabhoy, G., Van Dyke, M.W. Biochemistry (2005) [Pubmed]
  7. Development of distamycin-related DNA binding anticancer drugs. Marchini, S., Broggini, M., Sessa, C., D'Incalci, M. Expert opinion on investigational drugs. (2001) [Pubmed]
  8. Comparison of cell-cycle phase perturbations induced by the DNA-minor-groove alkylator tallimustine and by melphalan in the SW626 cell line. Erba, E., Mascellani, E., Pifferi, A., D'Incalci, M. Int. J. Cancer (1995) [Pubmed]
  9. Tallimustine lesions in cellular DNA are AT sequence-specific but not region-specific. Herzig, M.C., Trevino, A.V., Arnett, B., Woynarowski, J.M. Biochemistry (1999) [Pubmed]
  10. Estimation of the haematological toxicity of minor groove alkylators using tests on human cord blood cells. Ghielmini, M., Bosshard, G., Capolongo, L., Geroni, M.C., Pesenti, E., Torri, V., D'Incalci, M., Cavalli, F., Sessa, C. Br. J. Cancer (1997) [Pubmed]
  11. Hematopoietic toxicity and cell cycle perturbations induced by new DNA minor groove-alkylating agents. Filippini, C., Bisiach, M., Tagliabue, G., D'Incalci, M., Ubezio, P. Int. J. Cancer (1997) [Pubmed]
  12. Phase I study of the novel distamycin derivative tallimustine (FCE 24517). Sessa, C., Pagani, O., Zurlo, M.G., de Jong, J., Hofmann, C., Lassus, M., Marrari, P., Strolin Benedetti, M., Cavalli, F. Ann. Oncol. (1994) [Pubmed]
  13. Brostallicin (PNU-166196)--a new DNA minor groove binder that retains sensitivity in DNA mismatch repair-deficient tumour cells. Fedier, A., Fowst, C., Tursi, J., Geroni, C., Haller, U., Marchini, S., Fink, D. Br. J. Cancer (2003) [Pubmed]
  14. Accumulation of gamma-globin mRNA and induction of erythroid differentiation after treatment of human leukaemic K562 cells with tallimustine. Bianchi, N., Chiarabelli, C., Borgatti, M., Mischiati, C., Fibach, E., Gambari, R. Br. J. Haematol. (2001) [Pubmed]
  15. Decreased tyrosine phosphorylation in tumour cells resistant to FCE 24517 (tallimustine). Ciomei, M., Pastori, W., Capolongo, L., Geroni, C., Melegaro, G., Pennella, G., Grandi, M. Br. J. Cancer (1995) [Pubmed]
  16. Sequence-specific DNA alkylation of novel tallimustine derivatives. Marchini, S., Cozzi, P., Beria, I., Geroni, C., Capolongo, L., D'Incalci, M., Broggini, M. Anticancer Drug Des. (1998) [Pubmed]
  17. Cinnamoyl nitrogen mustard derivatives of pyrazole analogues of tallimustine modified at the amidino moiety: design, synthesis, molecular modeling and antitumor activity studies. Baraldi, P.G., Beria, I., Cozzi, P., Geroni, C., Espinosa, A., Gallo, M.A., Entrena, A., Bingham, J.P., Hartley, J.A., Romagnoli, R. Bioorg. Med. Chem. (2004) [Pubmed]
  18. Effects of a novel DNA-damaging agent on the budding yeast Saccharomyces cerevisiae cell cycle. Popolo, L., Viganò, F., Erba, E., Mongelli, N., D'Incalci, M. Yeast (1996) [Pubmed]
  19. Alpha-bromoacryloyl derivative of distamycin A (PNU 151807): a new non-covalent minor groove DNA binder with antineoplastic activity. Marchini, S., Cirò, M., Gallinari, F., Geroni, C., Cozzi, P., D'Incalci, M., Broggini, M. Br. J. Cancer (1999) [Pubmed]
  20. Tallimustine is inactive in patients with previously treated small cell lung cancer. A phase II trial of the National Cancer Institute of Canada Clinical Trials Group. Viallet, J., Stewart, D., Shepherd, F., Ayoub, J., Cormier, Y., DiPietro, N., Steward, W. Lung Cancer (1996) [Pubmed]
  21. Determination of tallimustine in human plasma by high-performance liquid chromatography. Marrari, P., Pianezzola, E., Strolin Benedetti, M. J. Chromatogr. B, Biomed. Appl. (1996) [Pubmed]
  22. DNA minor groove binding ligands: a new class of anticancer agents. D'Incalci, M., Sessa, C. Expert opinion on investigational drugs. (1997) [Pubmed]
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