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Journals and Conferences
Glucose-conjugated malonato-platinum(II) complexes are designed and synthesized to target tumor-specific active transporters, namely, glucose transporters (GLUTs); the complexes exhibit much higher aqueous solubility by 150 times, improved potency in cytotoxicities by 10 times, and increased therapeutic index by over 30 fold compared to the newest… (More)
Malignant neoplasms exhibit a higher rate of glycolysis than normal cells; this is known as the Warburg effect. To target it, a galactose-conjugated (trans-R,R-cyclohexane-1,2-diamine)-2-chloromalonato-platinum(II) complex (Gal-Pt) was designed, synthesized, and evaluated in five human cancer cell lines and against two different xenograft tumour models.… (More)
The main challenges currently encountered in chemotherapy are the lack of tumor selectivity and drug resistance. The design of novel cytostatic drugs has become the state-of-the-art technology in terms of targeted tumor therapy. This review illustrates the mechanisms and the advantages of representative chemotherapeutic agents, and presents an updated… (More)
An intramolecular C(sp(3))-O bond formation has been achieved via PhI(OAc)2/NaN3-mediated oxygenation of N,N-diaryl tertiary amines. The appealing features of this method include mild reaction conditions, absence of heavy-metal catalysts, and the direct intramolecular functionalization of sp(3) C-H bonds adjacent to nitrogen.
A group of functionalized oxazoles were synthesized in moderate to good yields from enamides via phenyliodine diacetate (PIDA)-mediated intramolecular cyclization. The main advantageous features of the present method include its broad substrate scope and the heavy-metal-free characteristic of the oxidative carbon-oxygen bond formation process.
The series of 3-monofunctionalized 2-oxindoles 2 were conveniently synthesized from reactions between anilide 1 and phenyliodine(III) diacetate (PIDA) through hypervalent iodine mediated C(sp2)–C(sp2) bond formation followed by a subsequent deacylation reaction. This metal-free method, shown to provide direct access to an important oxindole intermediate,… (More)
Treatment of β-monosubstituted enamines with phenyliodine bis(trifluoroacetate) (PIFA) was found to give a variety of 4,5-disubstituted 2-(trifluoromethyl)oxazoles. This approach allows the incorporation of the trifluoromethyl moiety in PIFA into the final products, which presumably takes place via the oxidative β-trifluoroacetoxylation of the enamine… (More)
An efficient ring-contraction reaction of isochromeno[4,3-b]indol-5(11H)-ones via a nucleophile-induced disproportionation/spirocyclization cascade process has been developed under mild conditions. The process realized the conversion of isochromeno[4,3-b]indol-5(11H)-ones into N-unsubstituted spiro[indoline-2,1'-isobenzofuran]-3,3'-diones and… (More)
A series of functionalized indenes bearing 1,3-dicyano groups were synthesized from electron-rich α-aryl ketonitriles in the presence of K(3)Fe(CN)(6) and NaOAc, possibly through tandem process involving dimerization, heterolytic cleavage of carbon-carbon bond, intermolecular coupling, and the subsequent intramolecular cyclization. The 2-arylindene… (More)