Ri-Zhen Huang

ORCID: 0000-0001-6651-5259
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About
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Research Areas
  • Synthesis and biological activity
  • Natural product bioactivities and synthesis
  • Metal complexes synthesis and properties
  • Phytochemistry and Biological Activities
  • Cancer therapeutics and mechanisms
  • X-ray Diffraction in Crystallography
  • Crystallization and Solubility Studies
  • Biological Activity of Diterpenoids and Biflavonoids
  • Click Chemistry and Applications
  • Ferrocene Chemistry and Applications
  • Bioactive natural compounds
  • Synthesis and Characterization of Heterocyclic Compounds
  • Phytochemical compounds biological activities
  • Bioactive Compounds and Antitumor Agents
  • Tryptophan and brain disorders
  • NF-κB Signaling Pathways
  • Organophosphorus compounds synthesis
  • Cancer Mechanisms and Therapy
  • Pharmacological Effects of Natural Compounds
  • Toxin Mechanisms and Immunotoxins
  • Synthesis of Organic Compounds
  • Drug Transport and Resistance Mechanisms
  • Berberine and alkaloids research
  • Adenosine and Purinergic Signaling
  • Plant biochemistry and biosynthesis

Guilin Medical University
2020-2025

Beibu Gulf University
2025

Guangxi Normal University
2013-2023

Southeast University
2016-2020

Fudan University
2016

Developing multifunctional platinum(IV) prodrugs via integrating bioactive pharmacophores into one entity is an attractive strategy to ameliorate the defects of platinum(II) drugs. Herein, a series indole-chalcone derivative-ligated complexes were synthesized and evaluated for their anticancer activities. Among them, optimal complex 17a exerted superior activity compared that cisplatin (CDDP) against tested cells but showed lower cytotoxicity toward human normal lung cells. Detailed...

10.1021/acs.jmedchem.2c02036 article EN Journal of Medicinal Chemistry 2023-03-22

Although cisplatin has been widely used for clinical purposes, its application is limited due to obvious side effects. To mitigate the defects of cisplatin, here, six "multitarget prodrugs" were synthesized by linking and NF-κB inhibitors. Notably, complex 9 demonstrated a 63-fold enhancement in activity against A549/CDDP cells with lower toxicity toward normal LO2 compared cisplatin. Additionally, could effectively cause DNA damage, induce mitochondrial dysfunction, generate reactive oxygen...

10.1021/acs.jmedchem.3c02182 article EN Journal of Medicinal Chemistry 2024-04-04

Three new Pt(IV) complexes comprising a combretastatin A-4 analogue were designed and synthesized. The resulting antitumor could significantly improve the antiproliferative activity overcome drug resistance of cisplatin in vitro. Interestingly, these novel compounds not only can carry DNA binding Pt(II) warhead into cancer cells but also have small molecule fragment that inhibit tubulin polymerization. Among them, complex 13, which was attached to an inhibitor at one axial position...

10.1021/acs.bioconjchem.6b00353 article EN Bioconjugate Chemistry 2016-08-05

Promising targeted therapy options to overcome drug resistance and side effects caused by platinum(II) drugs for treatment in hepatocellular carcinoma are urgently needed. Herein, six novel multifunctional platinum(IV) complexes through linking agents glycyrrhetinic acid (GA) were designed synthesized. Among them, complex 20 showed superior antitumor activity against tested cancer cells including cisplatin than simultaneously displayed good liver-targeting ability. Moreover, can...

10.1021/acs.jmedchem.4c00144 article EN Journal of Medicinal Chemistry 2024-05-10

A novel class of platinum(IV) complexes comprising a monoaminophosphonate ester moiety, which can not only act as bone-targeting group but also inhibit matrix metalloproteinases (MMPs), were designed and synthesized. Biological assay these compounds showed that they had potent antitumor activities against the tested cancer cell lines compared with cisplatin oxaliplatin indicated low cytotoxicity to human normal liver cells. Particularly, very sensitive resistant lines. The corresponding...

10.1021/acs.bioconjchem.7b00117 article EN Bioconjugate Chemistry 2017-03-09

Indoleamine-2,3-dioxygenase 1 (IDO1) and signal transducer activator of transcription 3 (STAT3) are important targets in the tumor microenvironment for cancer therapy. In present study, a set naphthoquinone aromatic amide-oxime derivatives were designed, which stimulated immune response via IDO1 inhibition simultaneously displayed powerful antitumor activity against three selected cell lines through suppressing STAT3 signaling. The representative compound 8u bound effectively to IDO1, with...

10.1021/acs.jmedchem.9b01386 article EN Journal of Medicinal Chemistry 2020-01-30

Acquired resistance in cancer remains a significant challenge oncology, posing obstacles to the efficacy of diverse therapeutic approaches. The nuclear factor-kappa B (NF-κB) signaling pathway plays an important role development drug tumor cells. Herein, we employed NF-κB inhibitors and cisplatin synthesize multitarget Pt(IV) antitumor prodrugs. Among them, antiproliferation activity complex 8 demonstrated remarkable 146.92-time increase compared against A549/CDDP Moreover, could effectively...

10.1021/acs.jmedchem.4c02840 article EN Journal of Medicinal Chemistry 2025-02-20
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