Abstract
A series of aroylnaphthalene derivatives were prepared as bioisosteres of combrestatin A-4 and evaluated for anticancer activity. 2-Amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalene, 9 and 8, respectively, showed strong antiproliferative activity with IC 50 values of 2.1-26.3 nM against a panel of human cancer cell lines including multiple-drug resistant cell line. Compound 9 demonstrated better antiproliferative activity and has a comparable tubulin binding efficacy as that of colchicine.
| Original language | English |
|---|---|
| Pages (from-to) | 8163-8167 |
| Number of pages | 5 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 51 |
| Issue number | 24 |
| DOIs | |
| Publication status | Published - 2008 Dec 25 |
Fingerprint
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Drug Discovery
Cite this
}
Synthesis and structure-activity relationships of 2-amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents. / Reddy, Gadarla Randheer; Kuo, Ching Chuan; Tan, Uan Kang; Coumar, Mohane Selvaraj; Chang, Chi Yen; Chiang, Yi Kun; Lai, Mei Jung; Yeh, Jiann Yih; Wu, Su Ying; Chang, Jang-Yang; Liou, Jing Ping; Hsieh, Hsing Pang.
In: Journal of Medicinal Chemistry, Vol. 51, No. 24, 25.12.2008, p. 8163-8167.Research output: Contribution to journal › Article
TY - JOUR
T1 - Synthesis and structure-activity relationships of 2-amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents
AU - Reddy, Gadarla Randheer
AU - Kuo, Ching Chuan
AU - Tan, Uan Kang
AU - Coumar, Mohane Selvaraj
AU - Chang, Chi Yen
AU - Chiang, Yi Kun
AU - Lai, Mei Jung
AU - Yeh, Jiann Yih
AU - Wu, Su Ying
AU - Chang, Jang-Yang
AU - Liou, Jing Ping
AU - Hsieh, Hsing Pang
PY - 2008/12/25
Y1 - 2008/12/25
N2 - A series of aroylnaphthalene derivatives were prepared as bioisosteres of combrestatin A-4 and evaluated for anticancer activity. 2-Amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalene, 9 and 8, respectively, showed strong antiproliferative activity with IC 50 values of 2.1-26.3 nM against a panel of human cancer cell lines including multiple-drug resistant cell line. Compound 9 demonstrated better antiproliferative activity and has a comparable tubulin binding efficacy as that of colchicine.
AB - A series of aroylnaphthalene derivatives were prepared as bioisosteres of combrestatin A-4 and evaluated for anticancer activity. 2-Amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalene, 9 and 8, respectively, showed strong antiproliferative activity with IC 50 values of 2.1-26.3 nM against a panel of human cancer cell lines including multiple-drug resistant cell line. Compound 9 demonstrated better antiproliferative activity and has a comparable tubulin binding efficacy as that of colchicine.
UR - http://www.scopus.com/inward/record.url?scp=58149096782&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=58149096782&partnerID=8YFLogxK
U2 - 10.1021/jm8008635
DO - 10.1021/jm8008635
M3 - Article
VL - 51
SP - 8163
EP - 8167
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 24
ER -