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5- (substituted phenyl) synthesis and antitumor activity of -2H- pyran derivatives of -2-

Author: LiXinChun
Tutor: XuYongNan
School: Shenyang Pharmaceutical University
Course: Medicinal Chemistry
Keywords: 2H-Pyran-2-one Suzuki cross-coupling reaction Anti-tumor
CLC: R914
Type: Master's thesis
Year: 2007
Downloads: 26
Quote: 0
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Abstract


2H-Pyran-2-one is a six-membered cyclic unsaturated ester that shares chemical properties reminiscent of alkene and aromatic compounds. It is highly abundant in bacteria, microbial, plant, insect and animal systems and takes parts in many different types of biological processes, such as defence against other organisms, as key biosynthetic intermediates, and as metabolites. Historically, 2/-/-pyran-2-ones are used as precursors for the synthesis of biologically important compounds such as pheromones, solanopyrones,α-chymotrysin, elastase, coumarins and analogues.Natural product SK-F12 is a 5-substituted 2H-Pyran-2-one with an IC50 value of 0.0014μg/mLin the inhibition of A549. Basing on the biological activity of 2H-Pyran-2-one, Twenty-seven compounds of 5-（substitutedphenyl）-2H-pyran-2-ones were designed and synthesized, twenty-two compounds of which are innovative and have not been reported yet. All the structures of the compounds were identified by 1H-NMR, MR and IR. The cytotoxic activities of these compounds against tumor cell（A549）were evaluated and cisplatin （PDD） was the positive control. Anti-tumor activity screens in vitro showed that PED-9 (IC50=2.05μg/mL) and PED-25 (IC50=7.48μg/mL) inhibited good inhibition of A549. Further pharmacological tests researches are underway.

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CLC: > Medicine, health > Pharmacy > Drug basic science > Medicinal Chemistry
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