NARKUNAN, Kesavaram,CHEN, Xinghai,KOCHAT, Harry,HAUSHEER, Frederick
申请号:
HUE07852779
公开号:
HUE031374T2
申请日:
2007.10.16
申请国别(地区):
HU
年份:
2017
代理人:
摘要:
The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<;600).