TY - JOUR
T1 - Synthesis, characterization, bioactivity, and POM analyses of isothiochromeno[3,4-e][1,2]oxazines
AU - Bennani, Brahim
AU - Kerbal, Abdelali
AU - Baba, Bouchra F.
AU - Daoudi, Maria
AU - Warad, Ismail
AU - Aljofan, Mohamad
AU - Alafeefy, Ahmed M.
AU - Masand, Vijay
AU - Hadda, Taibi B.
N1 - Funding Information:
Acknowledgments This work was supported by the grants from the Ministry of Education of Morocco (PGR-UMP-BH-2005 and PRO-TARS I). We are indebted to the National Cancer Institute (NCI) of the United States for biologic tests.
PY - 2013/10/1
Y1 - 2013/10/1
N2 - A series of 18 new 3,4-disubstituted-isothiochromeno[3,4-e][1,2]oxazines 28-45 has been obtained from the 3′,4′-di-substituted-4′H- spiro[isothiochromene-3,5′-isoxazol]-4(1H)-ones 10-27 in refluxing HCl acid/ethanol. A series of 15/18 compounds 28-45 was selected by the National Cancer Institute (NCI, Bethesda, USA) and were evaluated against a full panel of 60 primary human tumor cell lines derived from nine human cancer types, all of which showed antiproliferative activity in the micromolar range. The most active compound number 37 (S722910) showed high potency against all the tested cell lines with a GI50 mean value in the range of 30-80 μM; TGI and LC50 values were 12-16 μM having positive response on 98 and 63 % of the tested cell lines (Breast-MCF7 and NCS-SF-268) respectively. Graphical Abstract: [Figure not available: see fulltext.]
AB - A series of 18 new 3,4-disubstituted-isothiochromeno[3,4-e][1,2]oxazines 28-45 has been obtained from the 3′,4′-di-substituted-4′H- spiro[isothiochromene-3,5′-isoxazol]-4(1H)-ones 10-27 in refluxing HCl acid/ethanol. A series of 15/18 compounds 28-45 was selected by the National Cancer Institute (NCI, Bethesda, USA) and were evaluated against a full panel of 60 primary human tumor cell lines derived from nine human cancer types, all of which showed antiproliferative activity in the micromolar range. The most active compound number 37 (S722910) showed high potency against all the tested cell lines with a GI50 mean value in the range of 30-80 μM; TGI and LC50 values were 12-16 μM having positive response on 98 and 63 % of the tested cell lines (Breast-MCF7 and NCS-SF-268) respectively. Graphical Abstract: [Figure not available: see fulltext.]
KW - Breast cancer inhibition
KW - Leukemia
KW - POM analyses
KW - Spiro-isothiochromeno[3,4-e][1,2] oxazines
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U2 - 10.1007/s00044-012-0392-4
DO - 10.1007/s00044-012-0392-4
M3 - Article
AN - SCOPUS:84883464660
VL - 22
SP - 4798
EP - 4809
JO - Medicinal Chemistry Research
JF - Medicinal Chemistry Research
SN - 1054-2523
IS - 10
ER -