Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.

A series of novel substituted uracil-1'(N)-acetic acid esters (6-20) of camptothecins (CPTs) were synthesized by the acylation method. These new compounds were evaluated for in vitro antitumor activity against tumor cell lines, A549, Bel7402, BGC-823, HCT-8 and A2780. In vitro results showed that most of the derivatives exhibited comparable or superior cytotoxicity compare to CPT (1) and topotecan (TPT, 2), with 12 and 13 possessing the best efficacy.

[Study on the preparation of rapid-dissoluted EGb droppills].

Objective: To study the formulation and technique of preparation of rapid-dissoluted EGb (Extract of Ginkgo biloba) droppills.

Method: Taking the dissolution percentage of total flavonoids in EGb and weight variation as index, the formulation and technique of EGb droppills were optimized by the orthogonal experiment.

Result: T50 was 3.