| 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=4257 ------>medlineContent= ------>unit=000 ------>insert_date=20050404 ------>iam=1 ------>update_date=None ------>author=??? ------>change_event=2 ------>ISSN= ------>authors_c= ------>score=420 ------>journal_name=J. Med. Chem. ------>paper_name=Concise Synthesis of 1-Aroylindoles and 3-Aroylindoles, Combretastatin A-4 Analogues, as a Novel Class of Potent Antitubulin Agents. ------>confirm_date=None ------>tch_id=093131 ------>pmid=15293996 ------>page1=4247 ------>fullAbstract=The synthesis and study of the structure-activity relationships of two new classes of synthetic antitubulin compounds based on 1-aroylindole and 3-aroylindole skeletons are described. Lead compounds 3, 10, and 14 displayed potent cytotoxicities with IC50 = 0.9-26 nM against human NUGC3 stomach, MKN45 stomach, MESSA uterine, A549 lung, and MCF-7 breast carcinoma cell lines. The inhibition of proliferation correlated with in vitro polymerization inhibitory activities. Structure-activity relationships revealed that 6-methoxy substitution of 3-aroylindoles and 5-methoxy substitution of 1-aroylindoles contribute to a significant extent for maximal activity by mimicking the para substitution of the methoxy group to the carbonyl group in the case of aminobenzophenones. Addition of a methyl group at the C-2 position on the indole ring exerts an increased potency. The 3,4,5-trimethoxybenzoyl moiety was necessary for better activity but not essential and can be replaced by 3,5-dimethoxybenzoyl and 3,4,5-trimethoxybenzyl moieties. We conclude that 1- and 3-aroylindoles constitute an interesting new class of antitubulin agents with the potential to be clinically developed for cancer treatment. ------>tmu_sno=None ------>sno=10650 ------>authors2=Chang YL ------>authors3=Guo FM ------>authors4=Chang CW ------>authors5=Chang JY ------>authors6=Lee SJ,.Hsieh HP ------>authors6_c= ------>authors=Liou JP ------>delete_flag=0 ------>SCI_JNo=None ------>authors2_c= ------>publish_area=0 ------>updateTitle=Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin 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 |