TY - JOUR
T1 - Structure-activity relationship study of growth inhibitory 2-styrylchromones against carcinoma cells
AU - Lin, Chen
AU - Lu, Pei Jung
AU - Yang, Chia Ning
AU - Hulme, Christopher
AU - Shaw, Arthur Y.
N1 - Funding Information:
Acknowledgments Financial support from the National Science Council of the Republic of China and Tamkang University to A. Y. Shaw is gratefully acknowledged.
PY - 2013/5
Y1 - 2013/5
N2 - The structure-activity relationship study of 2-styrylchromones against carcinoma cell growth is discussed in the present report. Taking advantage of 2-styrylchromone as a molecular template, a series of structural modifications was carried out and examined on several carcinoma cell lines. Interestingly, AGS cells exhibited more sensitivity in response to methoxy-bearing compounds, of which compound 23 (3,4,5-trimethoxy group on ring B) showed the most potent activity with a GI50 value of 1.3 μM. Surprisingly, as methoxy groups in 12 and 24-27 were demethylated to generate their hydroxyl counterparts 28-32, none of them displayed appreciable activity against all carcinoma cells. We further confirmed the pivotal role of rigidity for growth inhibitory activity between the rigid 12 and its flexible counterpart 33. Taken together, in the present report, we have clearly demonstrated the structure-activity relationship study of 2-styrylchromones targeting carcinoma cell growth.
AB - The structure-activity relationship study of 2-styrylchromones against carcinoma cell growth is discussed in the present report. Taking advantage of 2-styrylchromone as a molecular template, a series of structural modifications was carried out and examined on several carcinoma cell lines. Interestingly, AGS cells exhibited more sensitivity in response to methoxy-bearing compounds, of which compound 23 (3,4,5-trimethoxy group on ring B) showed the most potent activity with a GI50 value of 1.3 μM. Surprisingly, as methoxy groups in 12 and 24-27 were demethylated to generate their hydroxyl counterparts 28-32, none of them displayed appreciable activity against all carcinoma cells. We further confirmed the pivotal role of rigidity for growth inhibitory activity between the rigid 12 and its flexible counterpart 33. Taken together, in the present report, we have clearly demonstrated the structure-activity relationship study of 2-styrylchromones targeting carcinoma cell growth.
KW - 2-Styrylchromone
KW - Carcinoma cells
KW - Growth inhibition
KW - Structure-activity relationship study
UR - https://www.scopus.com/pages/publications/84879685580
UR - https://www.scopus.com/pages/publications/84879685580#tab=citedBy
U2 - 10.1007/s00044-012-0232-6
DO - 10.1007/s00044-012-0232-6
M3 - Article
AN - SCOPUS:84879685580
SN - 1054-2523
VL - 22
SP - 2385
EP - 2394
JO - Medicinal Chemistry Research
JF - Medicinal Chemistry Research
IS - 5
ER -