Scientific Publications

SG2000 Publications:

  1. Janjigian Y. et al. (2010). A phase I trial of SJG-136 (NSC#694501) in advanced solid tumors. Cancer Chemother Pharmacol 65:833–838
  2. Hochhauser D. et al. (2009). Phase I Study of Sequence-Selective Minor Groove DNA Binding Agent SJG-136 in Patients with Advanced Solid Tumors. Clin Cancer Res,15(6) 2140-2147
  3. Narayanaswamy M. et al. (2008). An assay combining high-performance liquid chromatography and mass spectrometry to measure DNA interstrand cross-linking efficiency in oligonucleotides of varying sequences. Anal Biochem. 374(1) 173-81
  4. Calcutt W. M. (2008), Determination of chemically reduced pyrrolobenzodiazepine SJG-136 in human plasma by HPLC-MS/MS: application to an anticancer phase I dose escalation study. J. Mass Spectrom. 43: 42–52
  5. Pepper C. et al. (2007). Fludarabine-mediated suppression of the excision repair enzyme ERCC1 contributes to the cytotoxic synergy with the DNA minor groove crosslinking agent SJG-136 (NSC 694501) in chronic lymphocytic leukaemia cells. Br. J. Cancer 97(2) 253-259
  6. Gallmeier E. et al. (2006). Targeted disruption of FANCC and FANCG in human cancer provides a preclinical model for specific therapeutic options. Gastroenterology 130 2145-2154
  7. Buhrow S.A. et al. (2006). LC-MS/MS assay and dog pharmacokinetics of the dimericpyrrolobenzodiazepine SJG-136 (NSC 694501). J Chromatogr. B 840 56-62
  8. Clingen P. H. et al. (2005). The XPF-ERCC1 endonuclease and homologous recombination contribute to the repair of minor groove DNA interstrand crosslinks in mammalian cells produced by the pyrrolo[2,1-c][1,4]benzodiazepine dimer SJG-136. Nucleic Acids Res 33(10) 3283-3291
  9. Martin C. et al. (2005). Sequence-selective interaction of the minor-groove interstrand cross-linking agent SJG-136 with naked and cellular DNA: footprinting and enzyme inhibition studies. Biochemistry 44 4135-4147
  10. Guichard S. M. et al. (2005). Influence of P-glycoprotein expression on in vitro cytotoxicity and in vivo antitumouractivity of the novel pyrrolobenzodiazepine dimer SJG-136. Eur J Cancer41 1811-1818
  11. Wilkinson G. P. et al. (2004). Preliminary pharmacokinetic and bioanalytical studies of SJG-136 (NSC 694501), a sequence-selective pyrrolobenzodiazepine dimer DNA-cross-linking agent. Invest New Drugs 22 231-240
  12. Hartley J. A. et al. (2004). SJG-136 (NSC 694501), a novel rationally designed DNA minor groove interstrand cross-linking agent with potent and broad spectrum antitumor activity. Part 1: cellular pharmacology, in vitro and initial in vivo antitumor activity. Cancer Research 64 6693-6699
  13. Pepper C. J. et al. (2004). The novel sequence-specific DNA cross-linking agent SJG-136 (NSC 694501) has potent and selective in vitro cytotoxicity in human B-cell chronic lymphocytic leukaemia cells with evidence of a p53-independent mechanism of cell kill. Cancer Research 64 6750-6755
  14. Alley M. C. et al. (2004). SJG-136 (NSC 694501), a novel rationally designed DNA minor groove interstrand cross-linking agent with potent and broad spectrum antitumor activity: Part 2: Efficacy evaluations. Cancer Research 64 6700-6706
  15. Reid J. M. et al. (2004). LC-MS/MS assay and rat pharmacokinetics and metabolism of the dimeric pyrrolobenzodiazepine SJG-136. Proc Amer. Assoc. Cancer Res. 45 A5408
  16. Schweikart K. et al. (2004). In vitro myelosuppression of SJG-136, a pyrrolobenzodiazepine dimer: comparison to bizelesin. Proc. Amer. Assoc. Cancer Res45 A2113
  17. Smellie M. et al. (2003). Sequence-selective recognition of duplex DNA through covalent interstrand cross-linking: kinetic and molecular modelling studies with pyrrolobenzodiazepine dimers. Biochemistry 42 8232-8239
  18. Gregson S. J. et al. (2001).Design, synthesis and evaluation of a novel pyrrolobenzodiazepine DNA-interactive agent with highly efficient cross-linking ability and potent cytotoxicity. J. Med. Chem. 44 737-748
  19. Adams L. J. et al. (1999). Molecular modelling of a sequence-specific DNA-binding agent based on the pyrrolo[2,1-c][1,4]benzodiazepines. Pharm Pharmacol Commun 5 555-560
  20. Puvvada M. S. et al. (1997). Inhibition of bacteriophage T7 RNA polymerase in vitro transcription by DNA-binding pyrrolo[2,1- c][1,4]benzodiazepines. Biochemistry 36 2478-2484
  21. Mountzouris J. A. et al. (1994). Comparison of a DSB-120 DNA interstrand cross-linked adduct with the corresponding bis-tomaymycin adducts—an example of a successful template-directed approach to drug design based upon the monoalkylating compound tomaymycin. J MedChem 37 3132-3140
  22. Jenkins T. C. et al. (1994). Structure of a covalent DNA minor-groove adduct with a pyrrolobenzodiazepine dimers—evidence for sequence-specific interstrand cross-linking. J. Med. Chem. 37 4529-4537
  23. Puvvada M. S. et al. (1993). A quantitative assay to measure relative DNA binding affinity of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) antitumor antibiotics based on inhibition of restriction endonuclease BamHI. Nucleic Acid Res. 21 3671-3675
  24. Thurston D.E. (1993). Advances in the study of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) antitumor antibiotics. In: Neidle S., Waring M. J. (eds.). Molecular Aspects of Anticancer Drug-DNA Interactions (The Macmillan Press Ltd). 54-88

SG2285 publications:

  1. Hartley et al. (2010). SG2285, a novel C2-aryl-substituted pyrrolobenzodiazepine dimer pro-drug with potent antitumor activity. Cancer Research in press
  2. Howard P.W. et al. (2009). Synthesis of a novel C2/C2′-aryl-substituted pyrrolo[2,1-c][1,4]benzodiazepine dimer prodrug with improved water solubility and reduced DNA reaction rate. Bioorganic & Medicinal Chemistry Letters 19 6463–6466

SG2274 (GWL-78) Publications:

  1. Kotecha M. et al. (2008). Inhibition of DNA binding of the NF-Y transcription factor by the pyrrolobenzodiazepine-polyamide conjugate GWL-78. Mol Cancer Ther. 7(5) 1319-1328
  2. Wells, G. et. al. (2006) Design, synthesis and biophysical and biological evaluation of a series of pyrrolobenzodiazepine–poly(N-methylpyrrole) conjugates. J. Med. Chem. 2006, 49, 5442-5461

AS-1-145 (Centanamycin) publications:

  1. Rayburn E. et. al. (2010). Enterohepatic circulation of indolecarboxamide ML-970 (NSC 716970), an investigative anticancer agent. AACR 101st Annual Meeting Apr 20, 2010, poster number 3605.
  2. Yanow S. K. et al. (2008).Potent antimalarial and transmission-blocking activities of centanamycin, a novel DNA-binding agent. J. Infect. Dis.197(4)527-534
  3. Purcell L.A. et al. (2008). Chemical attenuation of Plasmodium berghei sporozoites induces sterile immunity in mice. Infect. Immun. 76(3) 1193-1199

Chemistry and General Publications:

  1. Dyeison A. et. al. (2010) Structure-Activity Relationships of Monomeric C2-Aryl Pyrrolo[2,1 c][1,4]benzodiazepine (PBD) Antitumor Agents. J. Med. Chem., 53, 2927–2941
  2. Tiberghien A. C. et. al. (2008). An asymmetric C8/C80-tripyrrole-linked sequence-selective pyrrolo[2,1-c][1,4]benzodiazepine (PBD) dimer DNA interstrand cross-linking agent spanning 11 DNA base pairs. Bioorganic & Medicinal Chemistry Letters 18, 2073–2077
  3. Dyeison et. al. (2008) Solution Structure of a 2:1 C2-(2-Naphthyl) Pyrrolo[2,1-c][1,4]benzodiazepine DNA Adduct: Molecular Basis for Unexpectedly High DNA Helix Stabilization. Biochemistry, 47 (45), pp 11818–11829
  4. Dyeison et. al. (2007) Parallel Synthesis of a Novel C2-Aryl Pyrrolo[2,1-c][1,4]benzodiazepine (PBD) Library. J. Comb. Chem., 9 (3), pp 437–445
  5. Kang G.-D. et al. (2003). Synthesis of a novel C2-aryl substituted 1,2-unsaturated pyrrolobenzodiazepine. Chem Commun14 1688-1689
  6. Cooper N. et al. (2002). Synthesis of novel C2-aryl pyrrolobenzodiazepines (PBDs) as potential antitumour agents. Chem. Commun. 1764-1765
  7. Berry J. M. et al. (2002). Synthesis and biological evaluation of a N10-Psec substituted pyrrolo[2,1-c][1,4]benzodiazepine prodrug. Bioorg Med. Chem. Lett. 12 1413-1416
  8. Sagnou M. J. et al. (2000). Design and synthesis of novel pyrrolobenzodiazepine (PBD) prodrugs for ADEPT and GDEPT. Bioorg. Med. Chem. Lett.10 2083-2086