| Liou JP |
------>authors3_c= ------>paper_class1=1 ------>Impact_Factor=2.825 ------>paper_class3=2 ------>paper_class2=1 ------>vol=1 ------>confirm_bywho=amel ------>insert_bywho=jpl ------>Jurnal_Rank=26.8 ------>authors4_c= ------>comm_author= ------>patent_EDate=None ------>authors5_c= ------>publish_day=1 ------>paper_class2Letter=None ------>page2=1118 ------>medlineContent= ------>unit=G0100 ------>insert_date=20061213 ------>iam=1 ------>update_date=None ------>author=??? ------>change_event=4 ------>ISSN= ------>authors_c= ------>score=500 ------>journal_name=ChemMedChem ------>paper_name=Structure-Activity Relationship Studies of 3-Aroylindoles as Potent Antimitotic Agents ------>confirm_date=20081125 ------>tch_id=093131 ------>pmid=16952120 ------>page1=1106 ------>fullAbstract=The concise synthesis and structure-activity relationship (SAR) studies of 3-aroylindoles were carried out in an effort to improve the potency and solubility of anticancer drug candidate BPR0L075 (8) by exploring structure modifications through three regimens: substitution of the B ring, at the N1 position, and of the 3-carbonyl linker. The SAR information revealed that the methoxy group of the B ring could be replaced with an electron-donating group such as methyl (in compound 9) or N,N-dimethylamino (in compound 13) while retaining both strong cytotoxic and antitubulin activities. The introduction of amide (compounds 30-33) and carbamate (compounds 34-37) functionalities at the N1 position of 8 gave analogues with potent antiproliferative activities. The cytotoxic potency of 8 was improved by replacing the carbonyl group with sulfide (compound 41) or oxygen (compound 43), indicating that the carbonyl moiety is important but not essential. The N,N-dimethylamino derivative 13 not only displayed potent cytotoxicity and antitubulin activity, but also showed a markedly improved physicochemical profile relative to the parent compound. ------>tmu_sno=None ------>sno=14382 ------>authors2=Mahindroo N ------>authors3=Chang CW ------>authors4=Guo FM ------>authors5=Lee SW ------>authors6=Yeh TK, Tan UK, Kuo CC, Chang YW, Lu PH, Tung YS, ------>authors6_c= ------>authors=Liou JP ------>delete_flag=0 ------>SCI_JNo=None ------>authors2_c= ------>publish_area=0 ------>updateTitle=Structure-activity relationship studies of 3-aroylindoles as potent antimitotic agents. ------>language=2 ------>check_flag=None ------>submit_date=None ------>country=None ------>no= ------>patent_SDate=None ------>update_bywho=None ------>publish_year=2006 ------>submit_flag=None ------>publish_month=10 |