Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids.

The development of hybrid compounds led to the discovery of new pharmacologically active agents for some of the most critical diseases, including cancer. Herein, we describe a new series of oxadiazole-containing structures designed by a molecular hybridization approach. Penicillin derivatives and amino acids were linked to amino acid and aromatic moieties through the formation of a 1,2,4-oxadiazole ring.

A Penicillin Derivative Exerts an Anti-Metastatic Activity in Melanoma Cells Through the Downregulation of Integrin αvβ3 and Wnt/β-Catenin Pathway.

The synthetic triazolylpeptidyl penicillin derivative, named TAP7f, has been previously characterized as an effective antitumor agent and against B16-F0 melanoma cells. In this study, we investigated the anti-metastatic potential of this compound on highly metastatic murine B16-F10 and human A375 melanoma cells. We found that TAP7f inhibited cell adhesion, migration and invasion in a dose-dependent manner.

Antitumor activity of new chemical compounds in triple negative mammary adenocarcinoma models.

Aim: According to the need for the development of new anticancer agents, we have synthetized novel bioactive compounds and aimed to determine their antitumor action.

Materials & Methods: We describe studies evaluating the effect of 35 novel chemical compounds on two triple negative murine mammary adenocarcinoma tumors.

Results & Conclusion: Three compounds were selected because of their high antitumor activity and their low toxicity to normal cells.

A novel penicillin derivative induces antitumor effect in melanoma cells.

In this study, we explored the in-vitro and in-vivo mechanism of antitumor action of a novel synthetic nonantibiotic triazolylpeptidyl penicillin derivative, named TAP7f, on B16-F0 murine melanoma cells. In-vitro assays showed that TAP7f caused an inhibition of S phase progression and a concomitant decrease of the percentage of cells in G0/G1 phase. We also found that TAP7f treatment induced an apoptotic response characterized by an increase of the sub-G1 fraction of B16-F0 hypodiploid cells, the occurrence of cells with picnotic nuclei, and the detection of phosphatidylserine exposure on the outer side of the plasma membrane.

Efficient alkene synthesis on solid support using the Julia-Kocienski coupling.

An efficient application of the Julia-Kocienski coupling for the olefination of aldehydes with resin-bound benzothiazol-2-yl and 1-phenyl-1H-tetrazol-5-yl sulfones is described. Olefins is generally obtained in high overall yield for the six-reaction steps.