黃建智副教授

研究領域：Medicinal Chemistry, Drug Discovery

最高學歷：國立清華大學化學博士

E-mail：lukehuang@mail.nsysu.edu.tw

連絡電話：07-5252000 #7206

辦公室：IR6001

個人網頁： ORCID

經歷

國立嘉義大學應用化學系助理教授/副教授/教授

2012-2022

財團法人生物技術開發中心研究員

2005-2012

國際威林生化科技公司研究員

2003-2005

專業

小分子新藥開發、藥物化學、有機合成

學術榮譽

First-in-class Nek2/Hec1抑制劑臨床候選藥物T-1101 tosylate共同發明人，其通過美國FDA之IND申請(2016年)，目前正進行臨床試驗中。

國立中山大學新進教師獎勵

2023-2024

講授科目

• 藥物化學

• 藥物開發通論

• 抗癌藥物現狀與展望

• 分子藥物設計與合成

• 生技產業實務與應用

• 小分子結構鑑定之光譜技術

專利及專書

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).

期刊論文

Selected Publications

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

國科會計畫

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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黃建智 副教授

黃建智副教授