TY - JOUR
T1 - Synthesis of novel 6,6a,7,8-tetrahydro-5H-naphtho[1,2-e]pyrimido[4,5-b][1, 4]diazepines under microwave irradiation as potential anti-tumor agents
AU - Insuasty, Braulio
AU - García, Angélica
AU - Quiroga, Jairo
AU - Abonia, Rodrigo
AU - Nogueras, Manuel
AU - Cobo, Justo
N1 - Funding Information:
The authors wish to credit The Developmental Therapeutics Program (DTP) of the National Cancer Institute of the United States (U.S) for performing the screening of compounds. Authors thank to Colciencias, Universidad del Valle (Colombia) and the Consejería de Innovación, Ciencia y Empresa (Junta de Andalucía, Spain) , the Universidad de Jaén (project reference UJA_07_16_33 ) and Ministerio de Ciencia e Innovación (project reference SAF2008-04685-C02-02 ) for financial support.
PY - 2010/7
Y1 - 2010/7
N2 - A new series of 6,6a,7,8-tetrahydro-5H-naphtho[1,2-e]pyrimido[4,5-b][1,4] diazepines 4a-f and 5a-f were efficiently synthesized in good yields from the reaction of E-2-arylidene-1-tetralones 1 and the respective tri- or tetraaminopyrimidines 2 or 3 under microwave irradiation using DMF as solvent and catalytic amounts of BF3·OEt2. Six of the obtained compounds were selected and tested by the National Cancer Institute (NCI-USA) against 60 different tumor cell lines. In particular, compounds 5a, 5c and 5e presented remarkable anti-tumor activity against melanoma cancer in SK-MEL-5 cell line.
AB - A new series of 6,6a,7,8-tetrahydro-5H-naphtho[1,2-e]pyrimido[4,5-b][1,4] diazepines 4a-f and 5a-f were efficiently synthesized in good yields from the reaction of E-2-arylidene-1-tetralones 1 and the respective tri- or tetraaminopyrimidines 2 or 3 under microwave irradiation using DMF as solvent and catalytic amounts of BF3·OEt2. Six of the obtained compounds were selected and tested by the National Cancer Institute (NCI-USA) against 60 different tumor cell lines. In particular, compounds 5a, 5c and 5e presented remarkable anti-tumor activity against melanoma cancer in SK-MEL-5 cell line.
KW - Aminopyrimidines
KW - Antitumoral activity
KW - Arylidene-1-tetralones
KW - Microwave irradiation
KW - Naphtho[1,2-e]pyrimido[4,5-b][1,4] diazepines
UR - https://www.scopus.com/pages/publications/77954349581
U2 - 10.1016/j.ejmech.2010.03.004
DO - 10.1016/j.ejmech.2010.03.004
M3 - Article
C2 - 20356658
AN - SCOPUS:77954349581
SN - 0223-5234
VL - 45
SP - 2841
EP - 2846
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
IS - 7
ER -
