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Dr. Luke Jiann-Jyh Huang Associate Professor

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Dr. Luke Jiann-Jyh Huang  Associate Professor

Research Areas: Medicinal Chemistry, Drug Discovery

E-mail: lukehuang@mail.nsysu.edu.tw

Web Page: ORCID

Roome: IR6001

Tel: 07-5252000 ext. 7206

Positions & Employments
Professor, Department of Applied Chemistry, National Chiayi University, Taiwan 2021-2022
Associate Professor, Department of Applied Chemistry, National Chiayi University, Taiwan 2015-2021
Assistant Professor, Department of Applied Chemistry, National Chiayi University, Taiwan 2012-2015
Research Fellow, Development Center for Biotechnology, Taiwan 2005-2012
Research Fellow, Well-being Biochemical Corporation, Taiwan 2003-2005
Specialty
Drug Discovery, Medicinal Chemistry, and Organic Synthesis
Honors & Awards
Dr. Huang is the co-inventor of T-1101 tosylate, a first-in-class Nek2/Hec1 inhibitor currently in clinical trials. This drug candidate has received U.S. FDA Investigational New Drug Approval in 2016.
NSYSU New Faculty Award, Taiwan 2023-2024
Courses
• Medicinal Chemistry infectious pathogens and their drug resistance
• General Theory Of Drug Discovery
• Current Status And Perspectives Of Anticancer Drugs
• Molecular Drug Design And Synthesis
• Current And Future Prospects For The Innovative Biotechnology Industry
• Spectroscopic Identification of Small Molecule Drugs
Patents
Co-inventor of 28 patents
1. Hwu, J.-R.; Tsay, S.-C.; Lu, K.-L.; Huang, J.-J.; Hung, J.-T.; Yu, S.-F. Organometallic Complex. US 6,812,247; EP 1,394,169; TW I267377; DE 60219621 (US, EU, TW & DE). 
2. Huang, J.-J.; Chiang, C.-C.; Liu, C.; Lai, C.-L; Lin, S. F.; Lin, Y.-H.; Wang, R.-W.; Yang, S.-C.; Chang, J.-M.; Chuang, S.-H.; Chen, P. Indolinone compounds as kinase inhibitors. US 7,897,602; TW I530483 (US & TW). 
3. Lau, J.; Huang, J.-J. Modulators of HEC1 activity and methods therefor. US 8,946,268; US 9,409,902 (divisional); EP 2,547,676; CA 2,793,311; CN 103038231; CN 105906617 (divisional); JP 5825535; JP 6294277 (divisional); KR 10-1609856; AU 2011227398; AU 2014210678 (divisional); ES 2,557,465; RU 2,576,036; MX 346395 (US, EU, CA, CN, JP, KR, AU, ES, RU, & MX). 
4. Huang, J.-J.; Liao, C.-B.; Chen, P. Quinazoline compounds as kinase inhibitors. US 8,785,459; TW I557109 (US & TW). 
5. Huang, J.-J.; Chuang, S.-H.; Lee, Y.-S. E.; Lau, J.; Huang, Y.-L. Improved modulators of Hec1 activity and methods therefor. US 8,999,983; US 10,588,909 (divisional); EP 2,785,714; CN 104254534; JP 5970554; TW I640519; AU 2012345843, KR 10-1983585, MX 371378 (US, CN, JP, AU, KR, & MX).
6. Wu, R.-Y.; Chen, H.-L.; Wu, Y.-Y.; Huang, J.-J.; Lee, S.-S.; King, K-L. “GLP-1 Potentiators from Hedychium coronarium and Their Applications,” US 9,150,482; TW I478902 (US & TW).
Selected publication
1. Chiang, C.-C. /…/ Huang, J. J.* Discovery of pyrrole–indoline-2-ones as Aurora kinase inhibitors with a different inhibition profile. J. Med. Chem. 2010, 53, 5929–5941.
2. Lin, S. F. /…/ Huang, J.-J.* Synthesis and structure–activity relationship of 3-O-acylated (–)-epigallocatechins as 5α-reductase inhibitors. Euro. J. Med. Chem. 2010, 45, 6068–6076.
3. Chang, T.-Y. /…/ Huang, J.-J.*; Sha, C.-K.* Synthesis and antiproliferative activities of ottelione A analogues. ACS Med. Chem. Lett. 2012, 3, 1075–1080.
4. Lee, Y.-S. E.; /…/ Huang, J.-J.* Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties. J. Med. Chem. 2014, 57, 4098–4110.
5. Liu, C.-W. /…/ Huang, J.-J.* Design and synthesis of pyrrole–5-(2,6-dichlorobenzyl)sulfonylindolin-2-ones with C-3’ side chains as potent Met kinase inhibitors. RSC Adv. 2014, 4, 58990–58998.
6. Chuang, S.-H. /…/ Huang, J.-J.* Discovery of T-1101 tosylate as a first-in-class clinical candidate for Hec1/Nek2 inhibition in cancer therapy. Euro. J. Med. Chem. 2020, 191: 112118.
7. Lee, C.-I. /…/ Huang, J.-J.* Design and synthesis of 4-anilinoquinazolines as Raf kinase inhibitors. Part 1. Selective B-Raf/B-RafV600E and potent EGFR/VEGFR2 inhibitory 4-(3-hydroxyanilino)-6-(1H-1,2,3-triazol-4-yl)quinazolines. Bioorg. Chem. 2021, 109: 104715.
8. Hsueh, W.-Y. /…/ Huang, J.-J.* Copper(I)-catalyzed nitrile-addition/N-arylation ring-closure cascade: synthesis of 5,11-dihydro-6H-indolo[3,2-c]quinolin-6-ones as potent topoisomerase-I inhibitors. J. Med. Chem. 2021, 64, 1435–1453.
9. Huang, J.-J.* /…/ Chou, S.-Y.* Synthesis of spirocyclopropane-containing 4H-pyrazolo[1,5-a]indoles via alkylative dearomatization and intramolecular N-imination of an indole–O-(methylsulfonyl)oxime. Molecules 2023, 28, 6374.
研究計畫、國科會計畫、產學合作計畫
NSTC Grants
1. 2-(2-Phenylacetamido)benzamides之新穎串聯反應研究 NSTC 113-2113-M-110-011
2. 金屬催化串聯反應於合成全新與少見四環雜環之研究(2/2) NSTC 112-2113-M-110-019
3. 金屬催化串聯反應於合成全新與少見四環雜環之研究(1/2) MOST 111-2113-M-110-017
4. Benzofuro[3,2-c]quinolinones之新穎金屬催化串聯反應合成法開發與其作為G-四聯體穩定劑及第二型拓樸異構酶α亞型選擇性抑制劑之研究  MOST 110-2113-M-415-006
5. Indolo[2,3-c]quinolinones 與其類似四環雜環合成之金屬催化串聯反應開發 MOST 106-2113-M-415-002
6. 2,6-雙甲基-1-鹵苯與胺基唑之銅催化C–N耦合反應開發(2/2) MOST 105-2113-M-415-001
7. 2,6-雙甲基-1-鹵苯與胺基唑之銅催化C–N耦合反應開發(1/2) MOST 104-2113-M-415-002
8. 具雙雜環主結構之化合物合成與其抗癌活性評估 NSC 102-2113-M-415-005-MY2
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