A natural product-like JAK2/STAT3 inhibitor induces apoptosis of malignant melanoma cells

The JAK2/STAT3 signaling pathway plays a critical role in tumorigenesis, and has been suggested as a potential molecular target for anti-melanoma therapeutics. However, few JAK2 inhibitors were being tested for melanoma therapy. In this study, eight amentoflavone analogues were evaluated for their activity against human malignant melanoma cells. The most potent analogue, compound 1, inhibited the phosphorylation of JAK2 and STAT3 in human melanoma cells, but had no discernible effect on total JAK2 and STAT3 levels. A cellular thermal shift assay was performed to identify that JAK2 is engaged by 1 in cell lysates. Moreover, compound 1 showed higher antiproliferative activity against human melanoma A375 cells compared to a panel of cancer and normal cell lines. Compound 1 also activated caspase-3 and cleaved PARP, which are markers of apoptosis, and suppressed the anti-apoptotic Bcl-2 level. Finally, compound 1 induced apoptosis in 80% of treated melanoma cells. To our knowledge, compound 1 is the first amentoflavone-based JAK2 inhibitor to be investigated for use as an anti-melanoma agent.published_or_final_versio

Synthesis and X-ray crystal structure of (cis-PdCl2)2[Ph2PNH)(NH)CC6H4C(NH)(NHPPh2)]·6DMF

The interaction of 1,4-phenylenebis[N-(diphenylphosphino-N′,N′-bis(trimethylsily)amidine], (Ph2PN)[N(SiMe3)2]CC6H4C[N(SiMe3)2](PPh2), with 2 equaivalents of PdCl2(PhCN)2 in THF gives (cis-PdCl2)2[(Ph2PNH)(NH)CC6H4C(NH)(NHPPh2)] in moderate yield. The compound has C2 symmetry and has been fully characterized by analytical, spectroscopic and X-ray diffraction methods. © 1995.link_to_subscribed_fulltex

Synthesis and X-ray crystal structure of cis-(CO)4Cr[(Me3SiN)C(Ph)(NHPPh2)]

The interaction of (Ph2PN)C(Ph)[N(SiMe3)2] with one equivalent of C7H8Cr(CO)4 in diethyl ether gave cis-(CO)4Cr[(Me3SiN)C(Ph)(NHPPh2)] in good yield. The compound has been fully characterized by analytical, spectroscopic and X-ray diffraction methods. The NH proton of the bidentate iminophosphine ligand undergoes facile deuterium exchange with D2O at ambient temperature. A 1,3-silyl shift mechanism has been proposed for the formation of the product.link_to_subscribed_fulltex

αvβ3-Isoform specific erbium complexes highly specific for bladder cancer imaging and photodynamic therapy

2016-2017 > Academic research: refereed > Publication in refereed journal201804_a bcmaVersion of RecordPublishe

Excitation energy transfer in ruthenium (II)-porphyrin conjugates led to enhanced emission quantum yield and 1O2 generation

202308 bckwAccepted ManuscriptRGCOthersEPSRC, HKBU-HK PolyU Joint Research Programme; Prospective Joint Research ProjectPublishe

An amphiphilic ruthenium(II)-polypyridyl appended porphyrin as potential bifunctional two-photon tumor-imaging and photodynamic therapeutic agent

An amphiphilic porphyrin appended with a Ru(II)-polypyridyl complex (Ru-P) showing a moderate two-photon absorption cross-section (178.0 ± 26.8 GM), high singlet oxygen quantum yield and rapid cellular uptake was synthesized. In vitro study using human nasopharyngeal carcinoma cells showed that Ru-P exhibited a strong two-photon induced fluorescence upon uptake, lysosomal localization and potent two-photon induced cytotoxicity. These results show that Ru-P, which was designed to enhance its cellular uptake, can potentially be used as an efficacious bifunctional two-photon tumor-imaging and photodynamic therapeutic agent despite its moderate two-photon absorption cross-section. © 2009 Elsevier Inc. All rights reserved.link_to_subscribed_fulltex