IADR Abstract Archives

Designing of new cytotoxic tetrahydroisoquinolines against oral squamous cell carcinoma

Objective: We have previously reported the good relation between the structure of 1,2,3,4-tetrahydroisoquinolines (TQ) and their cytotoxicity against human oral squamous cell carcinoma (OSCC) and leukemia cell lines (Ishihara et al., ANTICANCER Res., 29: 2265-2272 2009).  According to the results, we carried out the designing of new TQ compounds with higher cytotoxicity against OSCC cell lines.

Method: The most stable configuration of TQ was calculated by CONFLEX 5 and MOPAC/PM5 method. Molecular designing of new compounds were performed by ACD/Structure Design Suite software.

Result: The number of TQ compounds substituted at 2-position, assumed by ACD/Structure Design Suite, amounted to 3984.  Next, 313 TQ compounds with the assumed octanol-water partition coefficients (Log P) of 2.0-2.3 were selected.  To make the future synthesis easier, the number of compounds was narrowed down to approximately 40.

Conclusion: Using the selected compounds, the determination of chemical descriptors (such as surface area, volume and length of the molecule, etc.) by CONFLEX/PM5, and the search of new promising compounds are underway.

Division: IADR/LAR General Session
Meeting: 2012 IADR/LAR General Session (Iguaçu Falls, Brazil)
Location: Iguaçu Falls, Brazil
Year: 2012
Final Presentation ID: 614
Abstract Category|Abstract Category(s): Pharmacology/Therapeutics/Toxicology
Authors
  • Ishihara, Mariko  ( Meikai University, Sakado, Saitama, N/A, Japan )
  • Sakagami, Hiroshi  ( Meikai University, Sakado, Saitama, N/A, Japan )
  • SESSION INFORMATION
    Poster Session
    Pharmacology/Therapeutics/Toxicology II
    06/21/2012