title: Synthesis and Biological Evaluation of Strictosamide Derivatives with Improved Antiviral and Antiproliferative Activities.
abstract: A series of novel derivatives of strictosamide were synthesized and biologically evaluated. Most of the new compounds exhibited improved activities than the parent compound strictosamide. Among them, compounds Ib and If possessed antiviral activities against influenza A virus (A/Jinan/15/90) with IC50 values of 4.12 and 12.35 μg/mL, respectively. Compound Ie possessed antiviral activity against respiratory syncytial virus (RSV) with an IC50 value of 9.58 μg/mL. Both compounds IIc and IId had moderate antiproliferative effects against five human cancer cell lines. The preliminary structure-activity relationships were also concluded. This study provides a promising new template with potential antiviral activity.
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing, 210009, China.
authors.forename: Zan
authors.initials: Z
authors.lastname: Li
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing, 210009, China.|Jiangsu Zeukov Pharmaceutical S&T. Inc, Jiangsu, Nanjing, 210017, China.|State Key Lab of New-tech for Chinese Medicine Pharmaceutical Process, Jiangsu, Lianyungang, 222001, China.
authors.forename: Zhaoliang
authors.initials: Z
authors.lastname: Li
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing, 210009, China.
authors.forename: Yunwei
authors.initials: Y
authors.lastname: Lin
authors.affiliation: Jiangsu Zeukov Pharmaceutical S&T. Inc, Jiangsu, Nanjing, 210017, China.|State Key Lab of New-tech for Chinese Medicine Pharmaceutical Process, Jiangsu, Lianyungang, 222001, China.
authors.forename: Zhaoqing
authors.initials: Z
authors.lastname: Meng
authors.affiliation: Jiangsu Zeukov Pharmaceutical S&T. Inc, Jiangsu, Nanjing, 210017, China.|State Key Lab of New-tech for Chinese Medicine Pharmaceutical Process, Jiangsu, Lianyungang, 222001, China.
authors.forename: Gang
authors.initials: G
authors.lastname: Ding
authors.affiliation: Jiangsu Zeukov Pharmaceutical S&T. Inc, Jiangsu, Nanjing, 210017, China.|State Key Lab of New-tech for Chinese Medicine Pharmaceutical Process, Jiangsu, Lianyungang, 222001, China.
authors.forename: Liang
authors.initials: L
authors.lastname: Cao
authors.affiliation: Jiangsu Zeukov Pharmaceutical S&T. Inc, Jiangsu, Nanjing, 210017, China.|State Key Lab of New-tech for Chinese Medicine Pharmaceutical Process, Jiangsu, Lianyungang, 222001, China.
authors.forename: Na
authors.initials: N
authors.lastname: Li
authors.affiliation: Jiangsu Zeukov Pharmaceutical S&T. Inc, Jiangsu, Nanjing, 210017, China.|State Key Lab of New-tech for Chinese Medicine Pharmaceutical Process, Jiangsu, Lianyungang, 222001, China.
authors.forename: Wenjun
authors.initials: W
authors.lastname: Liu
authors.affiliation: Jiangsu Zeukov Pharmaceutical S&T. Inc, Jiangsu, Nanjing, 210017, China.|State Key Lab of New-tech for Chinese Medicine Pharmaceutical Process, Jiangsu, Lianyungang, 222001, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Xiao
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing, 210009, China.
authors.forename: Xiaoming
authors.initials: X
authors.lastname: Wu
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing, 210009, China.
authors.forename: Jinyi
authors.initials: J
authors.lastname: Xu
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects*; D004285:Dogs; D056945:Hep G2 Cells; D006801:Humans; D009980:Influenza A virus; D007251:Influenza, Human / Q000188:drug therapy* / Q000378:metabolism; D061985:Madin Darby Canine Kidney Cells; D018357:Respiratory Syncytial Virus Infections / Q000188:drug therapy* / Q000378:metabolism; D012136:Respiratory Syncytial Viruses; D014748:Vinca Alkaloids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000998:Antiviral Agents; D014748:Vinca Alkaloids; C539462:strictosamide
keywords: SARs; antiproliferative effect; antiviral activity; derivatives; strictosamide