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).
申请公布号
WO2009051578(A1)
申请公布日期
2009.04.23
申请号
WO2007US22028
申请日期
2007.10.16
申请人
BIONUMERIK PHARMACEUTICALS, INC.;NARKUNAN, KESAVARAM;CHEN, XINGHAI;KOCHAT, HARRY;HAUSHEER, FREDERICK
发明人
NARKUNAN, KESAVARAM;CHEN, XINGHAI;KOCHAT, HARRY;HAUSHEER, FREDERICK