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 IC50 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 IC50 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
C2 - 19053773
AN - SCOPUS:58149096782
SN - 0022-2623
VL - 51
SP - 8163
EP - 8167
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 24
ER -
