TY - JOUR
T1 - Aplysinopsin analogs
T2 - Synthesis and anti-proliferative activity of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-diones
AU - Thirupathi Reddy, Y.
AU - Narsimha Reddy, P.
AU - Koduru, Srinivas
AU - Damodaran, Chendil
AU - Crooks, Peter A.
N1 - Funding Information:
This research was supported by NIH/National Cancer Institute Grant PO1 CA104457 .
PY - 2010/5/15
Y1 - 2010/5/15
N2 - A series of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-dione (3) analogs structurally related to aplysinopsin, and that incorporate a variety of substituents in both the indole and N-benzyl moieties have been synthesized under microwave irradiation and conventional heating methods These analogs were evaluated for their anti-proliferative activity against MCF-7 and MDA-231 breast cancer cell lines, and A549 and H460 lung cancer cell lines. Two analogs, 3f and 3j had IC50 values of 4.4 and 5.2 μM, respectively, compared to 5-fluorouracil (IC50 = 15.2 μM) against MCF-7 cells.
AB - A series of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-dione (3) analogs structurally related to aplysinopsin, and that incorporate a variety of substituents in both the indole and N-benzyl moieties have been synthesized under microwave irradiation and conventional heating methods These analogs were evaluated for their anti-proliferative activity against MCF-7 and MDA-231 breast cancer cell lines, and A549 and H460 lung cancer cell lines. Two analogs, 3f and 3j had IC50 values of 4.4 and 5.2 μM, respectively, compared to 5-fluorouracil (IC50 = 15.2 μM) against MCF-7 cells.
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U2 - 10.1016/j.bmc.2010.03.054
DO - 10.1016/j.bmc.2010.03.054
M3 - Article
C2 - 20403701
AN - SCOPUS:77953136824
VL - 18
SP - 3570
EP - 3574
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
SN - 0968-0896
IS - 10
ER -