Synthesis, Antiproliferative Effect and In Silico LogP Prediction of BIM-23052 Analogs Containing Tyr Instead of Phe.

(1) Background: Hydrophobicity (or lipophilicity) is a limiting factor in the ability of molecules to pass through cell membranes and to perform their function. The ability to efficiently access cytosol is especially important when a synthetic compound has the potential to become a drug substance. D-Phe-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr-NH (BIM-23052) is a linear analog of somatostatin with established in vitro GH-inhibitory activity in nanomolar (nm) concentrations and high affinity to different somatostatin receptors.

Synthesis, Anticancer Activity, Docking Calculations and Hydrolytic Stability Studies of Bioconjugates of Monofluorenated Analogue of BIM- 23052.

Background: The fight against cancer has started since its discovery and has not subsided to nowadays. Currently, the hybrid molecules have become a promising alternative to the standard chemotherapeutics for the treatment of multi-causal diseases, including cancers.

Objective: Herein, we report the synthesis, biological evaluation, mathematical docking calculations and hydrolytic stability of the new bioconjugates of monofluorinated analogues of BIM-23052, containing second pharmacophore naphthalimide, caffeic acid or the tripeptide Arg-Gly-Asp.