The novel C7-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).
