Total synthesis and biological evaluation of halipeptins A and D and analogues.

The marine-derived halipeptins A (1a) and D (1d) and their analogues 3a, 3d and 4a, 4d were synthesized starting from building blocks 10, 13, 14a or 14d, 15, and 16. The first strategy for assembling the building blocks, involving a macrolactamization reaction to form the 16-membered ring hydroxy thioamide 52d as a precursor, furnished the epi-isoleucine analogue (4d) of halipeptin D, whereas a second approach involving thiazoline formation prior to macrolactamization led to a mixture of halipeptins A (1a) and D (1d) and their analogues 3a, 3d (epimers at the indicated site) and 4a, 4d (epimers at the indicated site). The same route starting with D-Ala resulted in the exclusive formation of the epimeric halipeptin D analogue 3d. The synthesized halipeptins, together with the previously constructed oxazoline analogues 5d and 6d, were subjected to biological evaluation revealing anti-inflammatory properties for 1a, 1d, and 6d while being noncytotoxic against human colon cancer cells (HCT-116)

Ruthenium half-sandwich complexes as protein kinase inhibitors: Derivatization of the pyridocarbazole pharmacophore ligand

10.1039/b700433hOrganic and Biomolecular Chemistry581218-122

First molecular evidence for reassessing phylogenetic affinities between genets (Genetta) and the enigmatic genet-like taxa Osbornictis, Poiana and Prionodon (Carnivora, Viverridae)

International audienceThe subfamily Viverrinae is a composite group of carnivores comprising the large and plantigrade terrestrial civets (Civettictis, Viverricula and Viverra) and the slender and generally more arboreal genets and genet-like taxa (Genetta, Prionodon, Poiana, Osbornictis), both having Asiatic and African representatives. The problematic phylogenetic relationships between genets and genet-like taxa are addressed for the first time from a molecular perspective through complete cytochrome b gene sequences. We used a large taxonomic sample set including some very rare and crucial species such as Osbornictis piscivora, Poiana richardsonii (museum specimen material) and Genetta johnstoni. The results from parsimony, distance and maximum likelihood analyses do not support the monophyly of the Viverrinae and contradict previous morphological hypotheses. The Asiatic linsangs (Prionodon spp.) are excluded from the Viverrinae and represent either a basal Feliformia or Viverridae. The other genet-like taxa constitute a strongly supported monophyletic African group, in which the African linsang (represented by Poiana richardsonii) is a sister group to the genets. The aquatic genet Osbornictis piscivora is included within the latter clade, and the genus Osbornictis should be considered a junior synonym of Genetta. African and Asiatic terrestrial civets are monophyletic, but their phylogenetic affinities with the genet-like clade are inconclusive using our data set. On the basis of our molecular results, morphological convergences and adaptations to peculiar habitats and ways of life within genets and genet-like taxa are discussed

Early phases of a successful invasion: mitochondrial phylogeography of the common genet (Genetta genetta) within the Mediterranean Basin

The Mediterranean Basin, connected by cultural exchanges since prehistoric times, provides an outstanding framework to study species translo- cations. We address here the early phases of the successful invasion of the common genet (Genetta genetta), a small carnivoran supposedly introduced from Africa to Europe during historical times, by assessing mitochondrial nucleotide variability in 134 individuals from its native and invasive ranges. We identify four lineages within the native species range [northern Algeria, Peninsular Arabia, southern Africa and western Africa + Maghreb (including northern Algeria)], in contradiction with morpho- logical taxonomy. We propose that the co- occurrence in Maghreb of two divergent lineages (autochthonous and western African) is due to secondary contact through intermittent permeability of the Saharan belt during the Plio-Pleistocene. Estimates of coalescence time and genetic diversity, in concert with other available evidences in the literature, indicate that the origin of European populations of common genets is in Maghreb, possibly restricted to northern Algeria. The autoch- thonous mitochondrial lineage of Maghreb was the only contributor to the European pool, suggesting that translocations were associated to a cultural constraint such as a local use of the species, which might have artificially excluded the western African lineage. Haplotype network and nested clade analysis (NCA) provide evidence for independent events of introductions throughout Spain (Andalucia, Catalun˜ a, and the Balearic Isl.)—and, to a lesser extent, Portugal—acting as a ‘translocation hotspot’. Due to the reduced number of northern Algerian individuals belonging to the autochthonous mitochondrial line- age of Maghreb, it remains impossible to test hypotheses of historical translocations, although a main contribution of the Moors is likely. Our demographic analyses support a scenario of very recent introduction of a reduced number of individ- uals in Europe followed by rapid population expansion. We suggest that an exceptional combi- nation of factors including multiple translocations, human-driven propagation across natural barriers, and natural processes of colonization allowed by a wide ecological tolerance, promoted the successful spread of the common genet into EuropePeer reviewe