The arachidonic acid metabolizing enzymes cyclooxygenase-2 (COX-2) and lipoxygenases (LOXs) have been found to be implicated in a variety of cancers, including prostate cancer. To develop new therapeutic treatments, it therefore seemed interesting to design dual COX-2/5-LOX inhibitors. We report here the synthesis and in vitro pharmacological properties of diarylpyrazole derivatives that have in their structure key pharmacophoric elements to obtain optimal interaction with subsites of active pockets in both enzyme systems. Using a molecular modeling approach, a set of SAR data is proposed, highlighting the importance of the sulfonyl group of one of the aryl moieties in terms of proliferation inhibition and/or apoptosis induction.

The polymorphism and intersolubility of a series of palmitic, stearic and oleic triglycerides have been investigated in order to understand the thermal properties of fractions of natural fats. Results are shown for tripalmitin (PPP), 2‐stearo‐dipalmitin, (PSP) and 2‐oleo‐dipalmitin (POP); these molecules differ essentially in the number of carbons (P→S) and the degree of unsaturation of chains (S→O). The different polymorphic forms have been verified by variable temperature X‐ray powder diffraction. The organization of the fatty acid carbon chains in the most stable polymorphic form(β′ or β) has been studied by variable temperature NMR spectroscopy by means of the protons relaxation times T1, T2 and T1ϱ. The construction of binary phase diagrams (PPP‐PSP and PPP‐POP), from the data obtained by differential scanning calorimetry and X‐ray powder diffraction, shows the formation of solid solutions or monotectic interactions, according to the nature and the polymorphic form of the triglycerides. The kinetic of the very importantβ′→β transition has been analyzed by variable temperature powder X‐ray diffraction for PPP, and [PPP‐PSP] or [PPP‐POP] blends. The molecular interactions occurring between the mixed crystals have been explained, by applying the model of Avrami and by an empirical isolation method.