podophyllotoxin/sarcoma

The spin-labeled derivative of podophyllotoxin, N'-podophyllic acid-N-[3-(2,2,5,5-tetramethyl pyrrolinenyloxy)] semicarbazide (GP-11), was synthesized and tested for its antitumor activity against mouse transplantable tumors, Sarcoma-180, Hepatoma-A, P388 leukemia and Ehrlich ascites carcinoma. At

The tubulin-binding affinities of podophyllotoxin and 12 related compounds have been compared with the effectiveness of these drugs in three assays of antitumor activity: (1) The mastocytoma assay of inhibited tumor cell growth in vitro; (2) the 37 sarcoma assay of tumor remission in vivo; and (3)

Single and combination chemotherapies of VP 16-213, a new antitumor agent were evaluated for its antitumor effect against several murine tumors. Dose-dependent antitumor effects were observed when VP 16-213 was administered via any of the three routes, i.p., i.v. and orally, on days 1 and 5 after

VM-26, a semisynthetic podophyllotoxin, was tested for antitumor activity and clinical toxicity in 181 children. The drug was administered iv at weekly intervals, beginning at a dose of 130 mg/2/week. The dose was increased, as tolerated, after 3 and 6 weeks to 150 and 180 mg/m2/week, respectively.

Experimental studies on anticancer drug resistance have shown that cisplatin and alkylating agents have a very low level of cross resistance towards heterocyclic agents such as anthracyclines, podophyllotoxins and vinca alkaloids. Based on this and on the model of Goldie and Coldman protocols using

1-beta-Alkyl derivatives of 1-desoxypodophyllotoxin were synthesized, and their cytotoxicity and inhibitory effects on DNA topoisomerase II (Topo-II) and tubulin polymerization were examined. The reaction of epipodophyllotoxin derivatives (1a-c) with trimethylallylsilane in the presence of boron