IR@PKUHSC  > 北京大学药学院
Synthesis and biological activities of 2-oxocycloalkylsulfonamides
Li, Xinghai1; Yang, Xinling1; Liang, Xiaomei1; Kai, Zhenpeng1; Yuan, Huizu2; Yuan, Dekai1; Zhang, Jianjun1; Wang, Ruiqing3; Ran, Fuxiang3; Qi, Shuhua2; Ling, Yun1; Chen, Fuheng1; Wang, Daoquan1
关键词2-oxocycloalkylsulfonamide Fungicidal Activity Antitumor Activity Qsar
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry

A series of novel 2-oxocycloalkylsulfonamides ( 4) were synthesized and their structures confirmed by IR, H-1 NMR, and elemental analysis. The bioassay showed that they have fair to excellent fungicidal activities against Botrytis cinerea Pers and Sclerotinia sclerotiorum. Among them, compounds 4A(10), 4A(11), 4A(12), 4B(2), and 4B(3), the EC50 values of which were 2.12, 3.66, 3.96, 2.38, and 2.43 mu g/mL, respectively, displayed excellent fungicidal activity against B. cinerea Pers, and are comparable with commercial fungicide procymidone ( the EC50 value is 2.45 mu g/mL). 3D QSAR against B. cinerea Pers was studied, a statistically significant and chemically meaningful CoMFA model was developed and some compounds which have a high predicted activity were forecasted. In addition, the bioassay also showed that the compounds have good inhibitory activities against human tumor cells HL-60, BGC-823, Bel-7402 and KB. It is interesting to point out that the antitumor activities of compounds 4 are in accordance with their fungicidal activity to a great extent: compounds having relatively best antitumor activities ( 4A10, 4A11, 4A12, and 4B3) also displayed excellent fungicidal activity. (c) 2008 Elsevier Ltd. All rights reserved.

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作者单位1.China Agr Univ, Dept Appl Chem, Key Lab Pesticide Chem & Applicat Technol, Beijing 100094, Peoples R China
2.Chinese Acad Agr Sci, Inst Plant Protect, Beijing 100094, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China
Recommended Citation
GB/T 7714
Li, Xinghai,Yang, Xinling,Liang, Xiaomei,et al. Synthesis and biological activities of 2-oxocycloalkylsulfonamides[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2008,16(8):4538-4544.
APA Li, Xinghai.,Yang, Xinling.,Liang, Xiaomei.,Kai, Zhenpeng.,Yuan, Huizu.,...&Wang, Daoquan.(2008).Synthesis and biological activities of 2-oxocycloalkylsulfonamides.BIOORGANIC & MEDICINAL CHEMISTRY,16(8),4538-4544.
MLA Li, Xinghai,et al."Synthesis and biological activities of 2-oxocycloalkylsulfonamides".BIOORGANIC & MEDICINAL CHEMISTRY 16.8(2008):4538-4544.
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