title: Facile construction of pyrrolo[1,2-b]isoquinolin-10(5H)-ones via a redox-amination-aromatization-Friedel-Crafts acylation cascade reaction and discovery of novel topoisomerase inhibitors.
abstract: An efficient redox-amination-aromatization-Friedel-Crafts acylation cascade process from trans-4-hydroxyproline and 2-formylbenzoic acids has been developed for the synthesis of pyrrolo[1,2-b]isoquinolin-10(5H)-ones. Compound 3h was identified as a new potent dual topoisomerase I/II inhibitor.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, P. R. China. shengcq@hotmail.com zhangwnk@hotmail.com.
authors.forename: Shanchao
authors.initials: S
authors.lastname: Wu
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, P. R. China. shengcq@hotmail.com zhangwnk@hotmail.com.
authors.forename: Na
authors.initials: N
authors.lastname: Liu
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, P. R. China. shengcq@hotmail.com zhangwnk@hotmail.com.
authors.forename: Guoqiang
authors.initials: G
authors.lastname: Dong
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, P. R. China. shengcq@hotmail.com zhangwnk@hotmail.com.
authors.forename: Lin
authors.initials: L
authors.lastname: Ma
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, P. R. China. shengcq@hotmail.com zhangwnk@hotmail.com.
authors.forename: Shengzheng
authors.initials: S
authors.lastname: Wang
authors.affiliation: Department of Clinical Nutrition, Changhai Hospital, Second Military Medical University, 168 Changhai Road, Shanghai 200433, P. R. China.
authors.forename: Wencai
authors.initials: W
authors.lastname: Shi
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, P. R. China. shengcq@hotmail.com zhangwnk@hotmail.com and School of Pharmacy, East China University of Science and Technology, Shanghai 200237, P. R. China.
authors.forename: Kun
authors.initials: K
authors.lastname: Fang
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, P. R. China. shengcq@hotmail.com zhangwnk@hotmail.com.
authors.forename: Shuqiang
authors.initials: S
authors.lastname: Chen
authors.affiliation: School of Pharmacy, East China University of Science and Technology, Shanghai 200237, P. R. China.
authors.forename: Jian
authors.initials: J
authors.lastname: Li
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, P. R. China. shengcq@hotmail.com zhangwnk@hotmail.com.
authors.forename: Wannian
authors.initials: W
authors.lastname: Zhang
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, P. R. China. shengcq@hotmail.com zhangwnk@hotmail.com.
authors.forename: Chunquan
authors.initials: C
authors.lastname: Sheng
authors.affiliation: School of Pharmacy, East China University of Science and Technology, Shanghai 200237, P. R. China and Department of Chemistry and Chemical Biology, University of New Mexico, Albuquerque, NM87131-0001, USA. wwang@unm.edu.
authors.forename: Wei
authors.initials: W
authors.lastname: Wang