TY - JOUR
T1 - Structure-activity relationships of hybrid annonaceous acetogenins
T2 - Powerful growth inhibitory effects of their connecting groups between heterocycle and hydrophobic carbon chain bearing THF ring on human cancer cell lines
AU - Kojima, Naoto
AU - Fushimi, Tetsuya
AU - Tatsukawa, Takahiro
AU - Yoshimitsu, Takehiko
AU - Tanaka, Tetsuaki
AU - Yamori, Takao
AU - Dan, Shingo
AU - Iwasaki, Hiroki
AU - Yamashita, Masayuki
N1 - Funding Information:
In vitro antiproliferative activities of hybrid annonaceous acetogenins against human cancer cell lines were examined by the Screening Committee of New Anticancer Agents supported by a Grant-in-Aid for Scientific Research on Priority Area ‘Cancer’ from The Ministry of Education, Culture, Sports, Science and Technology, Japan (MEXT) . This work was supported in part by Grants-in-Aid for Young Scientists (B) [Nos. 21790113, 23790130 ], a Grant-in-Aid for Scientific Research (B) [No. 22390021 ] from Japan Society for the Promotion of Sciences (JSPS) , and MEXT-Supported Program for the Strategic Research Foundation at Private Universities , 2008–2012.
PY - 2013
Y1 - 2013
N2 - Five novel hybrid molecules of annonaceous acetogenins and insecticides targeting mitochondrial complex I were synthesized and their growth inhibitory activities against 39 human cancer cell lines were investigated. It was revealed that the connecting group between the N-methylpyrazole part and the hydrophobic alkyl chain bearing the THF ring influenced their biological activities significantly. Amide-connected analog 2, in particular, showed selective and very potent activity (<10 nM) against some cancer cell lines.
AB - Five novel hybrid molecules of annonaceous acetogenins and insecticides targeting mitochondrial complex I were synthesized and their growth inhibitory activities against 39 human cancer cell lines were investigated. It was revealed that the connecting group between the N-methylpyrazole part and the hydrophobic alkyl chain bearing the THF ring influenced their biological activities significantly. Amide-connected analog 2, in particular, showed selective and very potent activity (<10 nM) against some cancer cell lines.
KW - Annonaceous acetogenin
KW - Antitumor agent
KW - Chemical synthesis
KW - Structure-activity relationship
UR - http://www.scopus.com/inward/record.url?scp=84876005438&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84876005438&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2013.03.009
DO - 10.1016/j.ejmech.2013.03.009
M3 - Article
C2 - 23587837
AN - SCOPUS:84876005438
SN - 0223-5234
VL - 63
SP - 833
EP - 839
JO - CHIM.THER.
JF - CHIM.THER.
ER -
