TY - JOUR
T1 - Concise syntheses of 7-anilino-indoline-N-benzenesulfonamides as antimitotic and vascular disrupting agents
AU - Mehndiratta, Samir
AU - Chiang, Yi-Fang
AU - Lai, Mei-Jung
AU - Lee, Hsueh Yun
AU - Chen, Mei Chuan
AU - Kuo, Ching-Chuan
AU - Chang, Chi-Yen
AU - Chang, Jang-Yang
AU - Liou, Jing Ping
PY - 2014/9/1
Y1 - 2014/9/1
N2 - Described herein is the development of a novel series of 7-anilino-indoline-N-benzenesulfonamides, derived from ABT751 (1), as potent anticancer agents. Amongst the synthesized series, compounds 6, 12, 13, and 14 have shown comparable to better anticancer activity on comparing with compound 1. 7-(4-Cyanophenylamino)-1-(4-methoxybenzenesulfonyl)indoline (13) was found to be the most potent one with up to 6 fold better activity against KB, HT29, and MKN45 cancer cell lines with IC50 values of 49.7, 149, and 92 nM, respectively. Compound 13 was also found inhibiting multidrug resistant cancer cell lines, blocking cell cycle at G2/M phase, and inhibiting tubulin polymerization. Capillary disruption assay results revealed that compound 13 was able to disrupt formed capillaries in a concentration-dependent manner without affecting cell viability.
AB - Described herein is the development of a novel series of 7-anilino-indoline-N-benzenesulfonamides, derived from ABT751 (1), as potent anticancer agents. Amongst the synthesized series, compounds 6, 12, 13, and 14 have shown comparable to better anticancer activity on comparing with compound 1. 7-(4-Cyanophenylamino)-1-(4-methoxybenzenesulfonyl)indoline (13) was found to be the most potent one with up to 6 fold better activity against KB, HT29, and MKN45 cancer cell lines with IC50 values of 49.7, 149, and 92 nM, respectively. Compound 13 was also found inhibiting multidrug resistant cancer cell lines, blocking cell cycle at G2/M phase, and inhibiting tubulin polymerization. Capillary disruption assay results revealed that compound 13 was able to disrupt formed capillaries in a concentration-dependent manner without affecting cell viability.
KW - ABT751
KW - Antimitotic
KW - CA-4
KW - Vascular-disrupting agents
UR - http://www.scopus.com/inward/record.url?scp=84906935715&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84906935715&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2014.06.042
DO - 10.1016/j.bmc.2014.06.042
M3 - Article
C2 - 25059503
AN - SCOPUS:84906935715
SN - 0968-0896
VL - 22
SP - 4917
EP - 4923
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 17
ER -
