BackgroundThe high mortality rate of oral cancers has stimulated the search for effective herbal medicines and their pharmacological targets. Vernonia cinerea, a perennial tropical herb, is wildly used as a traditional folk medicine for treatment of intestinal diseases and various skin diseases ...
By inspiration of significant anti-cancer activity of our previously screened natural ergosterol peroxide (EP), a series of novel steroidal 5α,8α-endoperoxide derivatives 5a–d and 14a–f were designed, synthesized, and biologically evaluated for their in vitro anti-proliferative inhibitory an...
The structural dynamics and stability of inclusion complexes of mansonone E (ME) and H (MH) including their stereoisomers with various βCDs (methylated- and hydroxypropylated-βCDs) were investigated by classical molecular dynamics (MD) simulations and binding free energy calculations. The simu...
A concise, efficient and facile protocol for the synthesis of a variety of 4-methyl-7-aryl/heteroaryl coumarins has been developed by utilizing the palladium catalyzed Suzuki cross-coupling reaction of 4-methyl-7-nonafluorobutylsulfonyloxy coumarin with a wide range of electronically diverse bor...
A series of 4-phenylpyrrole derivatives D were designed, synthesized, and evaluated for their potential as novel orally available androgen receptor antagonists therapeutically effective against castration-resistant prostate cancers. 4-Phenylpyrrole compound 1 exhibited androgen receptor (AR) ant...
Novel N-triazolyl maleimide derivatives were synthesized by azide–alkyne Huisgen cycloaddition (1,3-dipolar cycloaddition) and tested for cytotoxicity against a cell line derived from human melanomas SK-Mel-28 and SK-Mel-103, and human umbilical vein endothelial cell lines (HUVEC). The 4l was c...
The first catalytic enantioselective Michael addition of deconjugated butyrolactams to N-arylmaleimides is developed with the help of a bifunctional tertiary aminosquaramide catalyst. Unlike the widely explored and structurally related vinylogous nucleophile – deconjugated butenolides, deconjug...
Without employing any transition metal, organic solvent and base, a facile, economical and environmentally friendly strategy has been developed for the α-hydroxylation of β-keto esters and β-keto amides with peroxides via radical cross-coupling reaction in water under open-air conditions. Thi...
Many organophosphorous esters synthesized for applications in industry, agriculture, or warfare irreversibly inhibit acetylcholinesterase, and acute poisoning with these compounds causes life-threatening cholinergic overstimulation. Following classical emergency treatment with atropine, an oxime...
We report the synthesis and optoelectronic properties of a series of symmetrical disubstituted derivatives containing bis 1,3,4-oxadiazole with thieno[2,3-b]thiophene backbone (3a–f). These novel compounds were synthesized by employing simple and convenient synthetic protocol using thieno[2,3-b...
Methodology has been sought towards obtaining a 2-chloro-1,4-naphthoquinone bearing hydroxyl groups in the adjoining ring for obtaining either kermesic or carminic acids. In the first of these objectives, kermesic acid has been synthesised from 6-chloro-2,5,8-trihydroxynaphtho-1,4-quinone by the...
IntroductionMalignacies are still a major public concern worldwide and despite the intensive search of new chemotherapeutic agents, treatment still remains a challenging issue. The present study was designed to evaluate the cytotoxicity of 2-acetyl-7-methoxynaphtho[2,3-b]furan-4,9-quinone (AMNQ)...
Silica tetrahedron (also called siloxane) is an important structure of clay minerals, the percentage of which influences the hydrophobicity, polarity and other surface properties on clay mineral surfaces. In this study, a novel method for surface wettability modification of talc through thermal ...
The fused filament fabrication (FFF) process is characterized by fast local temperature decrease. Such characteristic usually leads to lower crystallinity degree in final printed parts when semi-crystalline polymers are used. By melt-compounding poly(lactic acid) (PLA) with its nucleating agent ...
The Kováts indices of 2-thiaadamantane and its 4-mono- and 4,8-disubstituted homologues were determined at 190, 200 and 210° for all of the solutes used. Capillary columns with Apiezon L (non-polar phase) and polyphenyl ether 6 P5E (medium polar phase) were used.
The Z:E ratios for the trifluoroethanolysis at 25°C of the title mesylate, chloride, bromide, and iodide are 126, 1020, 2230, and 9680, respectively, whose logarithms are linearly correlated with MM2 steric energies and Hansch's Es values.
Two novel thiophene 3,4-disubstituted organic dyes with double acceptors at 2,5-position framework photosensitizers were carefully designed and synthesized for the dye sensitized solar cell (DSSC) application. In this submission, the influence of carbazole (Cz) and triphenylaime (NPh3) units sub...
2,6-Dimethylpyridine N-oxide consistently reacts with various silver(I) salts to generate coordination polymers in which the N-oxide oxygen bridges two silver atoms. The recently reported μ3-O,O,O bridging mode observed with pyridine N-oxide is suppressed due to the greater steric demand of the...
We report the use of alkynylsilanes for the regiocontrolled synthesis of pyrazoles from functionalised sydnones. The strategies outlined herein allow a range of pyrazoles to be accessed with substitution patterns that are otherwise not directly obtained with high selectivity by alkyne cycloaddit...
The reaction of 3-(2-aminophenylamino)-5,5-dimethyl-2-cyclohexen-1-one with alloxan results in 3,3-dimethyl-1,2,3,4,10,11-hexa- hydrospiro(1H-dibenzo[b,e][1,4]diazepine)-11,5’-pyrimidine-1,2’,4’,6’-tetraone or N-aminocarbonyl-1-(2-aminophenyl)-3-hydroxy- 6,6-dimethyl-2,4-dioxo-2,3,4,5,6,7-he...
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