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Citation: XUE Si-Jia, SHENG Jie-Feng, WANG Qing-Dong, CAI Zhi-Juan. Synthesis,Crystal Structure and Antitumor Activity of α-L-Amino Acid Ester Derivatives[J]. Chinese Journal of Applied Chemistry, ;2008, 25(2): 152-156. shu

Synthesis,Crystal Structure and Antitumor Activity of α-L-Amino Acid Ester Derivatives

1.
College of Life and Environment Science, Shanghai Normal University, Shanghai 200234

Corresponding author: XUE Si-Jia,
Received Date: 15 January 2007
Available Online: 25 April 2007
Fund Project: 国家自然科学基金(20672073)资助项目 (20672073)上海市重点学科建设项目资助(T0402) (T0402)

In order to search for new antineoplastic drugs,nine novel N-2-thiophenesulfonyl-α-L-amino-acid esters were synthesized.The structures of the target compounds were determined by means of IR,¹H NMR,MS and elemental analysis.The crystal structure of the target compound 3a was determined by X-ray diffraction analysis.Crystal data:Monoclinic,space group:Cc,a=1.453 8(2) nm,b=0.569 02(9) nm,c=1.433 7(2) nm,Z=4,V=1.097 8(3) nm³,D_c=1.508 mg/m³,α=90.00°,β=112.245(2)°,γ=90.00°,F(000)=520,R=0.085 8,wR=0.226 5.Via MTT assay,the inhibitory rate of the title compounds against the K562 Cell Proliferation was measured.The inhibition rate of the compounds(3f,3g,3i) against leukemia K562 cell proliferation were 40.22%,33.47%,and 31.86%,respectively,when the concentration of was 1.0×10^-8 g/mL.The IC50 concentration(1×10^-6 g/mL) of the compounds(3a~3i) was 35.65,13.87,9.23,4.9,9.24,8.16,7.84,7.73,7.73,and 6.57,respectively.The result of preliminary bioassay shows that some of the target compounds possess antiproliferation effects on K562 cells.Some of the compounds induced cell apoptosis in the experiment.
- synthesis,
- α-L-amino-acid ester,
- K562 cell,
- thiophene-sulfonamide
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