title: Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents.
abstract: Twenty-five novel pyranochalcone derivatives were synthesized and evaluated for their in vitro and in vivo antiproliferative activities. Among them, compound 10i exhibited superior potent activity against 21 tumor cell lines including multidrug resistant phenotype with the IC50 values ranged from 0.09 to 1.30 μM. In addition, 10i significantly induced cell cycle arrest in G2/M phase, promoted tubulin polymerization into microtubules and caused microtubule stabilization. Further studies confirmed that 10i significantly suppressed the growth of tumor volume in HepG2 xenograft tumor model. Our study demonstrated that 10i could have beneficial antitumor activity as a novel microtubule stabilizing agent.
authors: State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Keyuan Road 4, Gaopeng Street, Chengdu 610041, China.
authors: Dong
authors: D
authors: Cao
authors: Xiaolei
authors: X
authors: Han
authors: Guangcheng
authors: G
authors: Wang
authors: Zhuang
authors: Z
authors: Yang
authors: Fei
authors: F
authors: Peng
authors: Liang
authors: L
authors: Ma
authors: Ronghong
authors: R
authors: Zhang
authors: Haoyu
authors: H
authors: Ye
authors: Minghai
authors: M
authors: Tang
authors: Wenshuang
authors: W
authors: Wu
authors: Kai
authors: K
authors: Lei
authors: Jiaolin
authors: J
authors: Wen
authors: Jinying
authors: J
authors: Chen
authors: Jingxiang
authors: J
authors: Qiu
authors: Xiaolin
authors: X
authors: Liang
authors: Yan
authors: Y
authors: Ran
authors: Yun
authors: Y
authors: Sang
authors: Mingli
authors: M
authors: Xiang
authors: Aihua
authors: A
authors: Peng
authors: Lijuan
authors: L
authors: Chen
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001578:Benzopyrans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D050150:Chalones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005260:Female; D056945:Hep G2 Cells; D006801:Humans; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D008870:Microtubules / Q000187:drug effects*; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013329:Structure-Activity Relationship; D050257:Tubulin Modulators / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C583785:2-methoxy-5-(3-(5-methoxy-2,2-dimethyl-2H-chromen-8-yl)-3-oxoprop-1-en-1-yl)phenyl propionate; D000970:Antineoplastic Agents; D001578:Benzopyrans; D050150:Chalones; D050257:Tubulin Modulators