Antitumor activities of some new 1,3,2-oxaza- and 1,3,2-diazaphosphorinanes against K562, MDA-MB-231, and HepG2 cells

作者：Gholivand Khodayar^*; Ghaziani Fatemeh; Shariatinia Zahra; Dorosti Nilufar; Mirshahi Manouchehr; Sarikhani Sina

来源：Medicinal Chemistry Research, 2012, 21(9): 2185-2195.

DOI：10.1007/s00044-011-9737-7

• 1,3,2-Oxazaphosphorinane
• Antitumor activity
• MTT assay
• K562
• MDA-MB-231
• HepG2

New X-substituted 1,3,2-oxazaphosphorinanes, where X = NHC6H5 (1), NHC6H4S(O)(2)NH2-4 (2), NHC6H4OCH3-4 (3), NHC6H4NO2-4 (4), OC6H4CH3-4 (5), NHC(O)C6H4NO2-4 (6), plus one X-substituted 1,3,2-diazaphosphorinane, where X = NHC6H4S(O)(2)NH2-4 (7), were synthesized and characterized by NMR, IR spectroscopy, and elemental analysis. The antitumor activities of these compounds, cyclophosphamide (CP), sulfanilamide (SA), and two X-substituted 5,5-dimethyl-1,3,2-diazaphosphorinanes, where X = NHC6H5 (8) OC6H4CH3-4 (9), were evaluated by cell culture on K562, MDA-MB-231, and HepG2 cell lines using MTT cell proliferation assay. The IC50 values for CP and compounds 1-9 were in the range of 0.06 mu M (for inhibition of HepG2 cells by compound 3) to 3.17 mu M (for inhibition of HepG2 cells by compound 8). It was found that compounds 2 and 7 containing sulfonamide substituent and also SA itself are the best candidates for antitumor activity very close to CP.

• 出版日期2012-9