1. Vehiculization of two novel
metal complexes to cancer cells
Andreu Paytuví Gallart

2. Introduction: cancer
Figurereferences:
FriedrichMarks.Cellular Signal Processing: An Introductiontothe MolecularMechanismsof Signal Transduction. Taylor&Francis Ltd. (2008).

3. Introduction: treatments
Novel metal
complexes
Figurereferences:
Kartalou,Maria; Essigmann,John M . Recognitionof cisplatin adductsby cellular proteins.Mutat. Res-Fun. Mol. M. 478, 1–21 (2001).

4. Introduction: bombesin
Bombesin:
Figurereferences:
Robinson,Clifford R.Reduce,reuse,andrecycle.Nature Biotechnology 20, 879 - 880 (2002).

5. Objectives
• Synthesis of bombesin analogs
• Attaching either complex K, complex CA323, or 5(6)-
carboxyfluorescein to bombesin analogs.
• DNA binding studies of complexes K and CA323.

6. Results: Design of bombesin analogs
Pyr
Met14

7. Results: Synthesis of bombesin analogues

8. Results: Synthesis of bombesin analogues incorporating the
complex CA323
APG-6-CA323
APG-9-CA323
APG-9-NLS-CA323

9. Results: Synthesis of bombesin analogues incorporating the
complex CA323

10. Results: Synthesis of bombesin analogues incorporating the
complex CA323

11. Results: Synthesis of bombesin analogues incorporating the
complex K
APG-9-(Complex K) (93% purity)
APG-9-NLS-(Complex K) (83% purity)

12. Results: Synthesis of 5(6)-carboxyfluorescein-labeled bombesin
analogs

13. Results: Attempts for the synthesis of 5(6)-carboxyfluorescein-
labeled bombesin analogs containing the metal complex CA323
None of them were obtained.

14. Results: binding studies
Secondroundof
electrophoresis
After24h
Secondroundof
electrophoresis
After48h
Thirdroundof
electrophoresis

15. Summary
• Bombesin analogs APG-6, APG-9, APG-9-Lys and APG-9-NLS.
– Synthesized in good to excellent purity (79-100%).
• Bombesin analog incorporating complex CA323, APG-9-(CA323).
– Synthesized in 57% purity.
• Bombesin analogs incorporating complex K, APG-9-(Complex K)
and APG-9-NLS-(Complex K).
– Synthesized in 93% and 83% respectively.
• 5(6)-carboxyfluorescein-labeled bombesin analogs APG-9-CF-Lys
and APG-9-Lys(CF).
– Synthesized in 69% and 100% purity, respectively.
• Neither complex K nor CA323 showed remarkable DNA interaction
under our working conditions.