The structural conformation of the tachykinin domain drives the anti-tumoural activity of an octopus peptide in melanoma BRAF.

Background And Purpose: Over past decades, targeted therapies and immunotherapy have improved survival and reduced the morbidity of patients with BRAF-mutated melanoma. However, drug resistance and relapse hinder overall success. Therefore, there is an urgent need for novel compounds with therapeutic efficacy against BRAF-melanoma.

Manganese(I) tricarbonyl complexes as potential anticancer agents.

The antiproliferative activity of [Mn(CO)(N^N)Br] (N^N = phendione 1, bipy 3) and of the two newly synthesized Mn complexes [Mn(CO)(acridine)(phendione)]OTf (2) and [Mn(CO)(di-triazole)Br] (4) has been evaluated by MTS against three tumor cell lines A2780 (ovarian carcinoma), HCT116 (colorectal carcinoma), HCT116doxR (colorectal carcinoma resistant to doxorubicin), and in human dermal fibroblasts. The antiproliferative assay showed a dose-dependent effect higher in complex 1 and 2 with a selectivity toward ovarian carcinoma cell line 21 times higher than in human fibroblasts. Exposure of A2780 cells to IC concentrations of complex 1 and 2 led to an increase of reactive oxygen species that led to the activation of cell death mechanisms, namely via intrinsic apoptosis for 2 and autophagy and extrinsic apoptosis for 1.

Triazole-Based Half-Sandwich Ruthenium(II) Compounds: From Antiproliferative Potential to Toxicity Evaluation.

A new series of half-sandwich ruthenium(II) compounds [(η-arene)Ru(L)Cl][CFSO] bearing 1,2,3-triazole ligands (arene = -cymene, L = (); arene = -cymene, L = (); arene = benzene, L = (); arene = benzene, (); = 2-[1-(-tolyl)-1-1,2,3-triazol-4-yl]pyridine and = 1,1'-di--tolyl-1,1'-4,4'-bi(1,2,3-triazole) have been synthesized and fully characterized by H and C NMR and IR spectroscopy, mass spectrometry, and elemental analysis. The molecular structures of , , and have been determined by single-crystal X-ray diffraction. The cytotoxic activity of - was evaluated using the MTS assay against human tumor cells, namely ovarian carcinoma (A2780), colorectal carcinoma (HCT116), and colorectal carcinoma resistant to doxorubicin (HCT116dox), and against normal primary fibroblasts.