| Liou JP |
------>authors3_c= ------>paper_class1=1 ------>Impact_Factor=5.076 ------>paper_class3=2 ------>paper_class2=1 ------>vol=47 ------>confirm_bywho=None ------>insert_bywho=jpl ------>Jurnal_Rank=8.3 ------>authors4_c= ------>comm_author= ------>patent_EDate=None ------>authors5_c= ------>publish_day=1 ------>paper_class2Letter=None ------>page2=2905 ------>medlineContent= ------>unit=000 ------>insert_date=20050404 ------>iam=1 ------>update_date=None ------>author=??? ------>change_event=2 ------>ISSN= ------>authors_c= ------>score=500 ------>journal_name=J. Med. Chem. ------>paper_name=Synthesis and Structure-Activity Relationships of 3-Aminobenzophenones as Antimitotic Agents. ------>confirm_date=None ------>tch_id=093131 ------>pmid=15139768 ------>page1=2897 ------>fullAbstract=A new series of 3-aminobenzophenone compounds as potent inhibitors of tubulin polymerization was discovered based on the mimic of the aminocombretastatin molecular skeleton. Lead compounds 5 and 11, with alkoxy groups at the C-4 position of B-ring, were potent cytotoxic agents and inhibitors of tubulin polymerization through the binding to the colchicine-binding site of tubulin. The corresponding antitubulin activities of 5 and 11 were similar to or greater than combretastatin A-4 and AVE-8063. Replacement of the methoxy group with a chloro group in the B ring of aminobenzopheneones (3, 8, and 9) caused drastic decrease in cytotoxic and antitubulin activity except in compounds 4 and 10, which could result from a unique alignment between chloro and amino groups located at the para position to each other. SAR information revealed that introduction of an amino group at the C-3 position in B ring of benzophenones, in addition to a methoxy group at the C-4 position, plays an important role for maximal cytotoxicity. ------>tmu_sno=None ------>sno=10646 ------>authors2=Chang JY ------>authors3=Chang CW ------>authors4=Chang CY ------>authors5=Mahindroo N ------>authors6=Hsieh HP ------>authors6_c= ------>authors=Liou JP ------>delete_flag=0 ------>SCI_JNo=None ------>authors2_c= ------>publish_area=0 ------>updateTitle=Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents. ------>language=2 ------>check_flag=None ------>submit_date=None ------>country=None ------>no= ------>patent_SDate=None ------>update_bywho=None ------>publish_year=2004 ------>submit_flag=None ------>publish_month=1 |