Journal of Pharmaceutical Sciences p. 852 - 858 (1994)
Update date:2022-09-26
Topics:
Dimmock
Sidhu
Chen
Li
Quail
Allen
Kao
A number of arylidene derivatives of alicyclic ketones and some corresponding oximes, oxime esters, and related compounds were prepared as candidate cytotoxic agents. All of the compounds were evaluated against murine L1210 lymphoid leukemia cells. In general, cytotoxicity was greatest with the α,β-unsaturated ketones and diminished with the oximes, and the oxime esters had little or no activity in this screen. When the same compounds were examined in both the in vitro L1210 and P388 leukemia screens, in the majority of cases the L1210 cells were more sensitive to these derivatives. Over half of the compounds prepared were evaluated against approximately 55 human tumors in vitro and showed selective toxicity toward one or more groups of neoplastic diseases, particularly leukemia. Some correlations between structure and bioactivity were discerned. The cytotoxicity screening and stability studies of representative compounds suggested that the ketones, oximes, and oxime esters were stable under the conditions of bioevaluation. X-ray crystallography of four representative compounds revealed structural features associated with cytotoxicity which may be considered in the design of future candidate cytotoxins.
View MoreSichuan Sangao Biochemical Co., Ltd
Contact:+86-28-84874233
Address:19F, Bldg.2, Shudu Center, Tianfu 2nd St., Hi-tech zone, Chengdu 610041, Sichuan Province, China.
Zhangjiagang Jianing Import & Export Co.,Ltd.
Contact:086-512-55379012 13913607595
Address:NO.1 Guotai North Road Zhangjiagang Economic Development Zone,215600,Jiangsu,China
Huangshi Shennong Chemical Technology Co., Ltd
Contact:+86-714-3072290
Address:Eastern industrial park , Tieshan district , Huangshi city ,Hubei province , China
Chemsky(shanghai)International Co.,Ltd.
Contact:0
Address:0
HEZE KINGVOLT CHEMICAL CO., LTD
Contact:86-573-82118911
Address:Juancheng Industry Park
Doi:10.1021/jo4014113
(2013)Doi:10.1021/jm00072a017
(1993)Doi:10.1002/jhet.1902
(2014)Doi:10.1016/0031-9422(93)85531-U
(1993)Doi:10.1016/S0040-4020(01)90163-2
(1993)Doi:10.3762/bjoc.9.240
(2013)