[Experimental study of the antitumor properties and mechanism of action of kortifen].

Cortiphen, a newly developed hormonal cytostatic ester of 11-desoxy-17 alpha-hydroxycorticosterone and chlorophenacyl, is described. It was studied in transplantable, spontaneous and induced tumors of 7 sites: hemoblastosis (5), hepatoma (3), mammary gland (5), lung (2), gastrointestinal tract (3), sarcoma (2) and melanoma. Practically all the tumors were shown to respond to cortiphen action.

[The antineoplastic activity of testiphenon].

The paper describes the antitumor activity of a newly-developed hormonocytostatic drug testiphenon--a complex ether of 5 alpha-dihydrotestosterone and chlorphenacyl (17 beta-[n-di/2-chloroethyl/aminophenylacetate]-5 alpha-androstan-17 beta-ol-3-on). Its antitumor properties were studied in 15 models of transplantable solid tumors and systemic neoplasms of mice and rats such as sarcoma 298, sarcoma 37, sarcoma-180, Lewis lung epidermoid carcinoma, carcinoma of the forestomach-5, large bowel adenocarcinoma, Harding-Passey's melanoma, cervical cancer-5, mammary adenocarcinoma Ca-755, hemoblastosis La, plasmacytoma MOPC-406, Rauscher's erythroblastosis, Walker's carcinosarcoma 256, sarcoma 45, alveolar carcinoma of the mammary gland and DMBA-induced mammary tumors of mice. The spectrum of antitumor activity of testiphenon proved wider than those of its components or other estrogeno-cytostatic drugs--phenestrol and estracyt.

[Alkylating derivatives of 2-amino-2-deoxysugars and 1-methylamino-1-deoxypolyols (synthesis and experimental study)].

A number of derivatives of 2-amino-2-deoxysaccharides and 1-methylamino-1-deoxypolyols acylated by cytotoxic phenylalkanic and amino acids were synthesized and experimentally tested for antitumor activity. Some compounds showed a high antitumor activity against plasmacytoma MOPC-406: a 2-fold increase in experimental animals survival and a 80--100% cure rate were observed. Physicochemical properties, particularly, stability in aqueous solution and antitumor activity of one of the most potent compounds--1-methylamino-1-deoxy-1-N[p-di(2-chloroethyl) aminophenylacetyl]-D-glucitol (Agluphen)--are described in detail.

[Properties of alkylating derivatives of estrogens].

The influence of phenestrol and XTJI-51 (hexestrol alkylating derivatives) on uterine tissues and their ability to bind to estrogen receptors were studied. The both compounds studied exhibited estrogenic properties and imitated all effects of estradiol: they increased the uterine wet weight and the activity of thymidine kinase and glucose-6-phosphate dehydrogenase. Although their affinity for estrogen receptors was much weaker than the affinity of estradiol, their complexes with estrogen receptors were more stable than estrogen-receptor complexes.

[Repair of DNA-protein cross-links induced by antineoplastic alkylating agents].

The bifunctional and antitumor alkylating agents embichin and its aromatic derivatives sarcolysin and chlorfenacyl remarkably differ in DNA-protein cross-links induction in Chinese hamster cell cultures in vitro. The differences involve the concentration necessary for cross-linkage, the time of cross-links emergence, and their reparation. Since all three compounds have the same alkylating group, it is obvious that the differences seen in the cross-linkage arise from the structure of aromatic groupings introduced into the molecule.