Application of organocatalysis in bioorganometallic chemistry: asymmetric synthesis of multifunctionalized spirocyclic pyrazolone–ferrocene hybrids as novel RalA inhibitors

Zhang, Yuehua; Wang, Chunting; Huang, Wei; Haruehanroengra, Phensinee; Peng, Cheng; Sheng, Jia; Han, Bo; He, Gu

doi:10.1039/c8qo00422f

Cited by 49 publications

(31 citation statements)

References 49 publications

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“…Derivative 72 (Fig. 6), as the most promising anticancer candidate, was designed and synthesized by Zhang and colleagues [56]. The consequence for ability of compound 72 inducing apoptotic death in PANC-1 cells showed that derivative 72 suppressed RalA according to inducing the accumulation of ROS and trigger mitochondrial apoptosis in PANC-1 cells.…”

Section: C-met Target Inhibitorsmentioning

confidence: 99%

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Zhao

Dai

et al. 2020

European Journal of Medicinal Chemistry

139

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a b s t r a c tThe pyrazolone structural motif is a critical element of drugs aimed at different biological end-points. Medicinal chemistry researches have synthesized drug-like pyrazolone candidates with several medicinal features including antimicrobial, antitumor, CNS (central nervous system) effect, anti-inflammatory activities and so on. Meanwhile, SAR (Structure-Activity Relationship) investigations have drawn attentions among medicinal chemists, along with a plenty of analogues have been derived for multiple targets. In this review, we comprehensively summarize the biological activity and SAR for pyrazolone analogues, wishing to give an overall retrospect and prospect on the pyrazolone derivatives.

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Section: C-met Target Inhibitorsmentioning

confidence: 99%

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Zhao

Dai

et al. 2020

European Journal of Medicinal Chemistry

139

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“…For western blotting, the total protein extracts from each sample were processed as previously described [72][73][74][75]. The total proteins were loaded into the SDS-PAGE (sodium dodecyl sulfate-polyacrylamide) gel and separated by their molecular weight via electrophoresis (PAGE).…”

Section: Western Blotting Analysismentioning

confidence: 99%

Novel HSP90-PI3K Dual Inhibitor Suppresses Melanoma Cell Proliferation by Interfering with HSP90-EGFR Interaction and Downstream Signaling Pathways

Zhao

Zhu

Xie

et al. 2020

IJMS

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Melanoma is the deadliest form of skin cancer, and its incidence has continuously increased over the past 20 years. Therefore, the discovery of a novel targeted therapeutic strategy for melanoma is urgently needed. In our study, MTT-based cell proliferation assay, cell cycle, and apoptosis assays through flow cytometry, protein immunoblotting, protein immunoprecipitation, designing of melanoma xenograft models, and immunohistochemical/immunofluorescent assays were carried out to determine the detailed molecular mechanisms of a novel HSP90-PI3K dual inhibitor. Our compound, named DHP1808, was found to suppress A375 cell proliferation through apoptosis induction by activating the Fas/FasL signaling pathway; it also induced cell-cycle arrest and inhibited the cell migration and invasion of A375 cells by interfering with Hsp90-EGFR interactions and downstream signaling pathways. Our results indicate that DHP1808 could be a promising lead compound for the Hsp90/PI3K dual inhibitor.

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“…In order to assess the possibility of subroutine cell death underlying 8m treatment, flow cytometry with annexinV/PI dual staining was used to assess the activation of apoptosis [39][40][41][42][43][44][45] . Hoechst 33258 staining also clearly showed that nuclear morphological changes in apoptotic cells, including chromatin condensation and apoptotic bodies, mediated apoptosis ( Figure 5(D)).…”

Section: Novel Hsp90/pi3ka Dual Inhibitors 8m Suppressed Cell B16 Melmentioning

confidence: 99%

Design, synthesis and molecular mechanisms of novel dual inhibitors of heat shock protein 90/phosphoinositide 3-kinase alpha (Hsp90/PI3Kα) against cutaneous melanoma

Qin

Wang

Jiang

et al. 2019

Journal of Enzyme Inhibition and Medicinal Chemistry

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Application of organocatalysis in bioorganometallic chemistry: asymmetric synthesis of multifunctionalized spirocyclic pyrazolone–ferrocene hybrids as novel RalA inhibitors

Abstract: Asymmetric construction of chiral spirocyclic pyrazolone–ferrocene hybrids has been developed. The lead compound displayed potent RalA inhibition.

Cited by 49 publications

References 49 publications

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Novel HSP90-PI3K Dual Inhibitor Suppresses Melanoma Cell Proliferation by Interfering with HSP90-EGFR Interaction and Downstream Signaling Pathways

Design, synthesis and molecular mechanisms of novel dual inhibitors of heat shock protein 90/phosphoinositide 3-kinase alpha (Hsp90/PI3Kα) against cutaneous melanoma

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