Simple and easy functionalization of -hydroxy POCOP-M (M = Ni(II), Pd(II)) pincer complexes: synthesis of multimetallic species.

A facile and efficient method for synthesizing mono- and bi-metallic pincer complexes (3-Ni/Ni and 3-Ni/Pd) has been developed. The procedure involves a 1 : 1 stoichiometric reaction of a -hydroxy POCOP pincer complex with cyanuric chloride in the presence of [NaB(OMe)], which selectively affords the mono-substituted pincer complexes (2-Ni and 2-Pd). These complexes are then further reacted with another equivalent of the -hydroxy POCOP pincer complex to produce the desired multimetallic species (3-Ni/Ni and 3-Ni/Pd).

Synthesis of Cycloartan-16β-ol from 16β 24R-Epoxy-Cycloartane and Their Cytotoxicity Evaluation Against Human Cancer Cell Lines.

It was found that Argentatins A and B triterpenoids make up approximately 20-30 % of the waste resin produced from the industrial processes to isolate rubber from P. argentatum. We have developed an efficient protocol for synthesizing cycloartane-16β-ol derivatives by opening the oxepane ring of argentatin B acetate (2) with BF-OEt.

Withanolides from Datura ceratocaula and Datura discolor and their acetylcholinesterase inhibitory activity.

The investigation of the chemical constituents of Datura ceratocaula and D. discolor allowed to isolate three new withanolides, datucerolide A (1) from the first species, and datudiscolides A (8) and B (9) from the second. In addition, seven known withanolides and five ubiquitous compounds were isolated from these plants, along with 27-O-β-d-glucopyranosyl dinnoxolide A (5), which was obtained as the tetraacetyl derivative 4.

Pentacoordinated Organotin(IV) Complexes as an Alternative in the Design of Highly Efficient Optoelectronic and Photovoltaic Devices: Synthesis and Photophysical Characterization.

The synthesis of four pentacoordinated organotin(IV) complexes prepared in a one-pot reaction from 2-hydroxy-1-naphthaldehyde, 2-amino-3-hydroxypyridine and organotin oxides is reported. The complexes were characterized by UV-Vis, IR, MS, H, C and Sn NMR techniques. The compound based on 2,2-diphenyl-6-aza-1,3-dioxa-2-stannanaphtho[1,2-h]pyrido[3,2-d]cyclononene revealed the formation of a monomeric complex with a distorted five-coordinated molecular geometry intermediate between the trigonal bipyramidal and square pyramidal.

Synthesis, biological evaluation, molecular docking studies and In-silico ADMET evaluation of pyrazines of pentacyclic triterpenes.

The semisynthesis of novel derivatives of lupeyl palmitate and 3β-palmitoyloxy-olean-12-ene by introduction of a pyrazine at C-2 / C-3 and modifications of the relatively unexplored C-30 position of lupeol derivatives was conducted, and their cytotoxic and anti-inflammatory activities were evaluated. The derivatives 7, 10 and 11 significantly inhibited the tumor cell lines U251, K562, HCT-15, MCF-7 and SKLU-1, and compounds 7 and 11 were more active (IC 25.4 ± 2.

Tyrame [N-(3-hydroxy-1:3:5(10)-estratrien-17β-yl)-4-hydroxy-phenethylamine], antithrombotic aminoestrogen that decreases microvesicle formation.

Background: Estrogens that are used as contraceptives or in replacement therapy are associated with an increase in the risk for developing thrombosis, mainly during the first year of treatment and in women with associated risk factors.

Objective: To synthesize, characterize and identify the anticoagulant, antiplatelet aggregation and microvesicle-reducing effect of the new aminoestrogen Tyrame.

Material And Methods: CD1 strain mice were used, which had Tyrame (0, 1 and 2 mg/100 g) subcutaneously administered.

Synthesis of flutamide-conjugates.

In this paper, we designed and extended modification basing on the flutamide structure. A series of flutamide-conjugates were obtained with methyl bromoacetate and ethylenediamine. Through the synthesis of two conjugates with 3,5-bis(dodecyloxy)benzoate derivatives, these flutamide conjugates were tested for anticancer activity.

Antifungal and antioomycete activities and modes of action of isobenzofuranones isolated from the endophytic fungus Hypoxylon anthochroum strain Gseg1.

Hypoxylon species are distributed worldwide and have been isolated from different habitats. The endophyte Hypoxylon anthochroum strain Gseg1 was isolated from healthy leaves of Gliricidia sepium. A chemical study of the culture medium and mycelium organic extracts of the endophytic fungus H.

Synthesis of Pt(II) complexes of the type [Pt(1,10-phenanthroline)(SArF)] (SArF = SCH-3,4-F; SCF-4-H; SCF). Preliminary evaluation of their in vitro anticancer activity.

A series of Pt(II) complexes of the type [Pt(1,10-phenanthroline)(SArF)] (SArF = SCH-3,4-F(1); SCF-4-H (2); SCF(3)) were synthesized from [Pt(1,10-phenanthroline)(Cl)] and [Pb(SArF)] via metathesis reactions. The complexes were fully characterized including the unambiguous determination of their molecular structures by single-crystal X-ray diffraction techniques, showing the metal centers to be into a slightly distorted square-planar environments. The in vitro cytotoxic activity of the complexes was evaluated on six cancerous cell lines, i.

Hopane-type triterpenes from Cnidoscolus spinosus and their bioactivities.

Chemical investigation of the aerial parts of Cnidoscolus spinosus resulted in the isolation of relatively infrequent hopane-type triterpenes, 3β-acetoxy-hop-22(29)-ene (1), first reported here as natural product, together with 3-oxo-hop-22(29)-ene (2), and 3β-hydroxy-hop-22(29)-ene (3). β-Amyrin palmitate and three phytosterols were also characterized. The structures of the compounds were established using spectroscopic methods, and those of 1 and 2 were confirmed by crystallographic analysis.

Structural Elucidation of Malonylcommunol and 6β-Hydroxy--communic Acid, Two Undescribed Diterpenes from . First Examples of Labdane Diterpenoids from a Mexican Species.

The aerial parts of afforded two undescribed labdane diterpenoids and (malonylcommunol and 6β-hydroxy--communic acid) along with two known labdane diterpenoids, -communic acid () and -communol (). Additionally, seven known metabolites were also isolated; two isopimarane diterpenoids and , two sesquiterpenoids identified as β-eudesmol () and cryptomeridiol (), and three aromatic compounds identified as phthalic acid (), a mixture of tyrosol fatty acid esters () and the flavone salvigenine (). While compounds compounds - showed significant inhibition of yeast α-glucosidase, compounds , and had no anti-inflammatory activity in the edema model induced by TPA.

The effect of chiral N-substituents with methyl or trifluoromethyl groups on the catalytic performance of mono- and bifunctional thioureas.

We evaluated thiourea organocatalysts that incorporate a chiral group which includes a trifluoromethyl moiety and contrasted their performance with non-fluorinated analogs. The comparison between such systems allows the direct study of the NH acidity of a thiourea bonded to an aliphatic substituent. In principle, -CF3 systems feature an enhanced hydrogen bond (HB) donor capacity that is undoubtedly beneficial for HB-catalysis applied to the Baylis-Hillman reaction.

Crystal structure and Hirshfeld surface analysis of -(5-iodo-4-phenyl-thia-zol-2-yl)acetamide.

Two crystallographically independent mol-ecules ( and ) are present in the asymmetric unit of the title compound, CHINOS, which differ mainly in the dihedral angle between the phenyl and thia-zole rings [38.94 (16) and 32.12 (15)°, respectively].

Cuautepestalorin, a 7,8-Dihydrochromene-Oxoisochromane Adduct Bearing a Hexacyclic Scaffold from Pestalotiopsis sp. IQ-011.

Cuautepestalorin (4), a 7,8-dihydrochromene-oxoisochromane adduct bearing a spiro-polycyclic (6/6/6/6/6/6) ring system, along with its putative biosynthetic precursors, cytosporin M (1), cytosporin N (2), and oxopestalochromane (3), were isolated from the bioactive extract of Pestalotiopsis sp. using a combination of molecular networking and dereplication techniques. Their structures were elucidated using a set of spectroscopic, spectrometric, chiroptical (experimental and theoretical), and X-ray crystallography data.

New Copper Compounds with Antiplatelet Aggregation Activity.

Background: Ischemic heart disease, cerebrovascular accident, and venous thromboembolism have the presence of a thrombotic event in common and represent the most common causes of death within the population.

Objective: Since Schiff base copper(II) complexes are able to interact with polyphosphates (PolyP), a procoagulant and potentially prothrombotic platelet agent, we investigated the antiplatelet aggregating properties of two novel tridentate Schiff base ligands and their corresponding copper( II) complexes.

Methods: The Schiff base ligands (L1) and (L2), as well as their corresponding copper(II) complexes (C1) and (C2), were synthesized and characterized by chemical analysis, X-ray diffraction, mass spectrometry, and UV-Visible, IR and far IR spectroscopy.

Hepatoprotective and Anti-Inflammatory Activities of the (Mc Vaugh) Leaf Extract in Chronic Models.

Previous report described that CHCl:MeOH extract of leaves and pure compounds (moretenol, moretenyl acetate, kaempferol-3,7-dimethyl ether, and 5-hydroxy-7-3',4'-trimethoxyflavanone) showed important topical and systemic anti-inflammatory activity in acute model, as well as antimycobacterial and antiprotozoal activities. In this paper, we describe the hepatoprotective and anti-inflammatory effects of the CHCl:MeOH extract in chronic model and the isolation of additional compounds (moretenone and lupeol acetate). The hepatoprotective activity was determined at 39 days using Balb/c mice with liver damage induced with an antitubercular drug (RIF/INH/PZA).

Anticancer Activity of Resorcinarene-PAMAM-Dendrimer Conjugates of Flutamide.

Methods: The synthesis of conjugates of flutamide with resorcinarene-PAMAM-dendrimers as well as alkyl and ethyl phenyl chains in the lower part of the macrocycle as a nucleus and diethylenetriamines in the dendritic branches gives the opportunity to obtain conjugates in one step of synthesis with 16 and 64 flutamide moieties in the structure.

Results: The in vitro anticancer studies showed that the conjugates of flutamide are more active than the free flutamide and the flutamide derivatives, thus diminishing the amount of flutamide used. The resorcinarenedendrimer- flutamide conjugates with a high drug payload improve the activity of the drug.

Crystal structure of ochraceolide A isolated from (Turcz.) Lundell.

The title compound, CHO [systematic name: 6a,6 b,8a,9a,12a,14b)-4,4,6a,6;b,8a,14b-hexa-methyl-12-methyl-eneicosa-hydro-3-phenanthro[1',2':6,7]indeno-[2,1-]furan-3,11(2)-dione], is a triterpene lactone, which was isolated from di-chloro-methane extract of (Turcz.) Lundell (celastraceae) stem bark. The compound has a lupane skeleton and consists of four fused six-membered rings and two five-membered rings.

Retro-Curcuminoids as Mimics of Dehydrozingerone and Curcumin: Synthesis, NMR, X-ray, and Cytotoxic Activity.

Curcumin and its derivatives have been extensively studied for their remarkable medicinal properties, and their chemical synthesis has been an important step in the optimization of well-controlled laboratory production. A family of new compounds that mimic the structure of curcumin and curcuminoids, here named -curcuminoids (-), was synthesized and characterized using 1D ¹H- and C-NMR, IR, and mass spectrometry; the X-ray structure of , , , , , , and are reported here for the first time. The main structural feature of these compounds is the reverse linkage of the two aromatic moieties, where the acid chloride moiety is linked to the phenolic group while preserving α, β-unsaturated ketone functionality.

neo-Clerodane Diterpenoids and Other Constituents of Salvia filipes.

A series of neo-clerodane-type diterpenoids were isolated from the aerial parts of Salvia filipes, including the new compounds 4-epi-polystachyne A (1), salvifilines A (3), C (7), and D (8), and salvifiline B, which was isolated as the 15-O-methyl derivatives 4/5. In addition, the five known diterpenoids (2, 9-12), together with ursolic, oleanolic, and betulinic acids, and the flavone eupatorin were also isolated. The structures were determined by analysis of their spectroscopic data, mainly 1D and 2D NMR.