A5103256651- Multicomponent Synthesis of Heterocycles
- Synthesis and biological activity
- Synthesis and Biological Evaluation
- Cancer-related molecular mechanisms research
- Ferroptosis and cancer prognosis
- NF-κB Signaling Pathways
- Bioactive Compounds and Antitumor Agents
- Cancer Immunotherapy and Biomarkers
- MicroRNA in disease regulation
- Natural product bioactivities and synthesis
- X-ray Diffraction in Crystallography
- PARP inhibition in cancer therapy
- Crystallization and Solubility Studies
- Cytokine Signaling Pathways and Interactions
- Click Chemistry and Applications
- RNA Interference and Gene Delivery
- Cancer, Stress, Anesthesia, and Immune Response
- Microbial Metabolism and Applications
- Tannin, Tannase and Anticancer Activities
- Histone Deacetylase Inhibitors Research
- Toxin Mechanisms and Immunotoxins
- Cardiovascular, Neuropeptides, and Oxidative Stress Research
- Natural Compounds in Disease Treatment
- Cancer therapeutics and mechanisms
- Adenosine and Purinergic Signaling
Tsinghua University
2022-2024
Tsinghua–Berkeley Shenzhen Institute
2022-2024
Chengdu University of Traditional Chinese Medicine
2022-2024
National Health Research Institutes
2016-2020
Taipei Medical University
2015-2016
National Kaohsiung Marine University
2009-2013
Targeted delivery and precise release of toxins is a prospective strategy for the treatment triple-negative breast cancer (TNBC), yet flexibility to incorporate both properties simultaneously remains tremendously challenging in X-drug conjugate fields. As critical components conjugates, linkers could flourish achieving optimal functionalities. Here, we pioneered pH-hypersensitive tumor-targeting aptamer AS1411-triptolide (AS-TP) achieve smart toxin targeted therapy against TNBC. The...
Epigenome aberrations have been observed in tobacco-associated human malignancies. (-)-epigallocatechin-3-gallate (EGCG) has proven to modulate gene expression by targeting DNA methyltransferases (DNMTs) through a proposed mechanism involving the gallate moiety of EGCG. We show that gallic acid (GA) changes methylome lung cancer and pre-malignant oral cell lines markedly reduces both nuclear cytoplasmic DNMT1 DNMT3B within 1 week. GA exhibits stronger cytotoxicity against line H1299 than...
Bioactive dihydropyrimidinones (DHPs) were designed and synthesized by a multicomponent Biginelli reaction. The reaction was catalyzed the polarized surface of nano-zirconium dioxide with partial positive charge 0.52e at Zr center negative −0.23e oxygen center. There good corroboration between computed experimental ZrO2 cell parameters bond distances as determined in silico vitro methods. Since DHPs found to target peroxisome proliferator-activated receptor (PPAR)-γ, we tested these ligands...
// Guihua Sun 1 , Ya-Wen Cheng 4 Lily Lai 2 Tsui-Chin Huang Jinhui Wang 3 Xiwei Wu Yafan Yasheng Jinghan Keqiang Zhang Shuya Hu Ji-Rui Yang and Yun Yen 1,4 Department of Molecular Pharmacology, Beckman Research Institute the City Hope, Duarte, CA, USA Surgery, Integrated Genome Core, Graduate Cancer Biology Drug Discovery, College Medical Science Technology, Taipei University, Taipei, Taiwan Correspondence to: Sun, email: Yen, Keywords : microRNA, colorectal cancer, small RNA deep...
In breast cancer (BC), STAT3 is hyperactivated. This study explored the design of imidazopyridine-tethered pyrazolines as a de novo drug strategy for inhibiting phosphorylation in human BC cells. involved synthesis and characterization two series compounds namely, 1-(3-(2,6-dimethylimidazo [1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-(4-(substituted)piperazin-1-yl)ethanone...
Small molecule-driven JNK activation has been found to induce apoptosis and paraptosis in cancer cells. Herein pharmacological effects of synthetic oxazine (4aS, 7aS)-3-((4-(4‑chloro-2-fluorophenyl)piperazin-1-yl)methyl)-4-phenyl-4, 4a, 5, 6, 7, 7a-hexahydrocyclopenta[e] [1,2]oxazine (FPPO; BSO-07) on JNK-driven demonstrated human breast (BC) MDA-MB231 MCF-7 cells respectively. BSO-07 imparted significant cytotoxicity BC cells, induced JNK, increased intracellular reactive oxygen species...
A number of uracil amides cleave poly (ADP-ribose) polymerase and therefore novel thiouracil amide compounds were synthesized screened for the loss cell viability in a human-estrogen-receptor-positive breast cancer line. The exhibited moderate to significant efficacy against human cells, where compound 5e IC50 value was found be 18 μM. Thouracil 5a inhibited catalytical activity PARP1, enhanced cleavage phosphorylation H2AX, increased CASPASE 3/7 activity. Finally, silico analysis...
Meta-analysis revealed that Leucine Zipper Down-Regulated In Cancer 1 (LDOC1) increased methylation more in people with lung tumors than those who were healthy and never smoked. Quantitative methylation-specific PCR cigarette smoke condensate (CSC) exposure drives LDOC1 promoter hypermethylation silence human bronchial cells. Immunohistochemistry studies showed downregulation is associated poor survival of patients cancer. Loss gain functions enhanced attenuated aggressive phenotypes...
Novel PARP inhibitors with selective mode-of-action have been approved for clinical use. Herein, oxadiazole based ligands that are predicted to target PARP-1 synthesized and screened the loss of cell viability in mammary carcinoma cells, wherein seven compounds were observed possess significant IC50 values range 1.4 25 µM. Furthermore, compound 5u, inhibited MCF-7 cells an value 1.4µM, when compared Olaparib (IC50 = 3.2 µM). Compound 5s also decreased MDA-MB-231 15.3 19.2 µM, respectively....
Small molecules are being used to inhibit cyclin dependent kinase (CDK) enzymes in cancer treatment. There is evidence that CDK a drug-target for therapy across many tumor types because it catalyzes the transfer of terminal phosphate ATP protein acts as substrate. Herein, identification pyranopyrazoles were inhibitors was attempted, whose synthesis catalyzed by nano-zirconium dioxide via multicomponent reaction. Additionally, we performed an in-situ analysis intermediates reactions,...
A highly efficient potassium carbonate-mediated [3 + 2] cycloaddition reaction of hydrazonoyl chlorides with cinnamic aldehydes to furnish multi-substituted pyrazoles under nontoxic and mild conditions has been developed. plausible stepwise mechanism is proposed. This protocol featured broad substrate coverage, good functional group tolerance, wide scalability, operational simplicity, as well conveniently constructed pyrazole scaffolds.
Our previous data showed that the Momordica grosvenori Swingle extract (MSE) exhibited anti-inflammatory effect through markedly suppressed LPS-induced up-regulation of inducible NO synthase (iNOS), cyclooxygenase-2 (COX-2) and ODC (ornithine decarboxylase) gene expression in RAW 264.7 cells. Regarding link between inflammation carcinogenesis, we further investigated bio-molecular mechanisms both anti-tumor activities vivo using a TPA (12-O-tetradecanoyl phorbol 13-acetate)-stimulated mouse...
Poor oral hygiene (POH) is associated with squamous cell carcinoma (OSCC). Oral microbes often proliferate due to POH. Array data show that LDOC1 plays a role in immunity against pathogens. We investigated whether regulates the production of microbe-induced IL-1β, an oncogenic proinflammatory cytokine OSCC. demonstrated presence Candida albicans (CA) 11.3% OSCC tissues (n = 80). CA and bacterium Fusobacterium nucleatum stimulate higher levels IL-1β secretion by LDOC1-deficient cells than...
Despite kinetic resolution (KR) via N-heterocyclic carbene (NHC)-catalyzed acylation minimizing any competitive racemic background reactions, the KR of NHC-activated lactam amidation is mostly uninvestigated.