Hui‐Hsia Hsieh
Current Organizations / Institutes
The organizations/institutes from the scholar's latest article
Research Subjects
Hui‐Hsia Hsieh has a total of 5 co-authors. Here are the top co-authors by number of shared publications:
- Hai-Anh Ha
Faculty of Pharmacy, College of Medicine and Pharmacy, Duy Tan University, Da Nang, Vietnam
1 shared publication - Kuo-Chu Lai
Department of Physiology and Pharmacology, College of Medicine Chang Gung University Taoyuan City Taiwan, ROC
1 shared publication - Mann-Jen Hour
School of Pharmacy, China Medical University, Taichung, Taiwan
1 shared publication - Shin-Yi Liu
Graduate Institute of Biomedical Sciences, College of Medicine, China Medical University, Taichung 40402, Taiwan
1 shared publication Yi‐Liang Lu
School of Pharmacy China Medical University Taichung City Taiwan, ROC
1 shared publication
Latest Publications
- 5 December 2025
- Published by Wiley in Chemical Biology & Drug Design
- Vol. 106 (6) , e70209
Design and Synthesis of Holu‐7, a Quinazolinone Derivative With an Active Stereo Geometry and Polar 2,4‐Dihydroxyphenyl Group, as a Selective Anticancer Agent
Quinazolin‐4‐one scaffolds offer rich anticancer chemistry but often trade potency for selectivity. Building on a tubulin‐targeting lead ( MJ‐65 ), 12 new derivatives ( 26 – 37 ) were synthesized to dissect geometry–activity relationships and enhance the polarity of C2‐substituents. Cytotoxicity was profiled against cancerous (HCT116 and CAL27) and normal (FHC) cells. In silico studies employed CDOCKER against tubulin (PDB 5NJH), GROMACS for molecular dynamics (MD), and ProTox‐3.0 for toxicity estimation. The previously synthesized geometry‐matched pairs 21 – 25 were active at 10 μM. In contrast, their isomers 26 – 30 were largely inactive, revealing a configuration‐dependent binding mechanism. Optimizing polarity yielded Holu‐7 (compound 35 ; 2,4‐dihydroxyphenyl at the C2‐position), which exhibited sub‐50 nM IC 50 in HCT116/CAL27 cells and > 10 μM in FHC cells and induced robust G 2 /M arrest. Docking/MD supported stable vinca‐site engagement, with hydrogen bonds to ASP179/ASN206 and π‐stacking with TYR224. ProTox‐3.0 predicted a higher LD 50 and absence of major organ toxicities relative to MJ‐65 . This data indicates that configuration‐aware, polarity‐tuned design can deliver selective quinazolinone anticancer candidates; therefore, Holu‐7 merits further preclinical evaluation.
- 5 December 2025
- Published by Wiley in Chemical Biology & Drug Design
- Vol. 106 (6) , e70209
Design and Synthesis of Holu‐7, a Quinazolinone Derivative With an Active Stereo Geometry and Polar 2,4‐Dihydroxyphenyl Group, as a Selective Anticancer Agent
Quinazolin‐4‐one scaffolds offer rich anticancer chemistry but often trade potency for selectivity. Building on a tubulin‐targeting lead ( MJ‐65 ), 12 new derivatives ( 26 – 37 ) were synthesized to dissect geometry–activity relationships and enhance the polarity of C2‐substituents. Cytotoxicity was profiled against cancerous (HCT116 and CAL27) and normal (FHC) cells. In silico studies employed CDOCKER against tubulin (PDB 5NJH), GROMACS for molecular dynamics (MD), and ProTox‐3.0 for toxicity estimation. The previously synthesized geometry‐matched pairs 21 – 25 were active at 10 μM. In contrast, their isomers 26 – 30 were largely inactive, revealing a configuration‐dependent binding mechanism. Optimizing polarity yielded Holu‐7 (compound 35 ; 2,4‐dihydroxyphenyl at the C2‐position), which exhibited sub‐50 nM IC 50 in HCT116/CAL27 cells and > 10 μM in FHC cells and induced robust G 2 /M arrest. Docking/MD supported stable vinca‐site engagement, with hydrogen bonds to ASP179/ASN206 and π‐stacking with TYR224. ProTox‐3.0 predicted a higher LD 50 and absence of major organ toxicities relative to MJ‐65 . This data indicates that configuration‐aware, polarity‐tuned design can deliver selective quinazolinone anticancer candidates; therefore, Holu‐7 merits further preclinical evaluation.