title: Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety.
abstract: We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed that some compounds exhibit broad-spectrum antitumor potency, and the most active compound23p(IC50: 2.357-3.012 μM) was found more potent than Sunitinib (IC50: 31.594-49.036 μM) against HepG2, A549 and Skov-3, respectively.
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. jun0215@126.com.|Zhejiang Starry Pharmaceutical Co. Ltd., Xianju 317300, China. jun0215@126.com.
authors.forename: Jun
authors.initials: J
authors.lastname: Zhang
authors.affiliation: Zhejiang Starry Pharmaceutical Co. Ltd., Xianju 317300, China. swy109@starrypharma.com.
authors.forename: Weiyi
authors.initials: W
authors.lastname: Shen
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. lxn18273645@163.com.
authors.forename: Xiaoning
authors.initials: X
authors.lastname: Li
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. yunchai18@126.com.
authors.forename: Yun
authors.initials: Y
authors.lastname: Chai
authors.affiliation: Zhejiang Starry Pharmaceutical Co. Ltd., Xianju 317300, China. lisj0966@163.com.
authors.forename: Senjun
authors.initials: S
authors.lastname: Li
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. lvkailk@hotmail.com.
authors.forename: Kai
authors.initials: K
authors.lastname: Lv
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. imbhyguo@126.com.
authors.forename: Huiyuan
authors.initials: H
authors.lastname: Guo
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. lmllyx@126.com.
authors.forename: Mingliang
authors.initials: M
authors.lastname: Liu
mesh_terms: D000072283:A549 Cells; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D000077210:Sunitinib
chemical_list: D000970:Antineoplastic Agents; D001372:Aza Compounds; D007211:Indoles; D011758:Pyrroles; D000077210:Sunitinib
keywords: 5-bromo-7-azaindolin-2-ones; antitumor activity; synthesis