Suppression of the immunological reaction by methylhydrazines,a new class of antitumour agents

Zusammenfassung 1-Methyl-2-p-(isopropylcarbamoyl)-benzyl-hydrazin-hydrochlorid (I), ein Cytostaticum, hemmt die Immunreaktion gegen heterologe Tumortransplantate. Diese Reaktion wird nur beeinträchtigt, wenn das Methylhydrazin-Derivat vor der Implantation gegeben wird. Die erwähnte Verbindung gehört einer Gruppe von neuen Cytostatica an, die unter anderem auch die Lymphopoese beeinflussen. Die Zusammenhänge zwischen der Wachstumshemmung gewisser mesenchymaler Gewebe (Lymphocyten, Plasmazellen etc.), der Beeinträchtigung der Antikörperproduktion bzw. der Unterdrückung der Immunreaktionen gegenüber fremden Geweben, werden diskutiert.     

Synthesis and antitumour activity of new daunorubicin and adriamycin analogues

Summary A new synthetic procedure for the preparation of daunorubicin and adriamycin analogues bearing different substituents on ring D, has been developed. The new compounds display outstanding efficacy against experimental tumours of mice.     

Synthesis and antitumour activity of new daunorubicin and adriamycin analogues

A new synthetic procedure for the preparation of daunorubicin and adriamycin analogues bearing different substituents on ring D, has been developed. The new compounds display outstanding efficacy against experimental tumours of mice.     

Glutamine aminotransferase and glutamine aminohydrolase ratio as a possible test for antitumour compounds.

Three known antitumour drugs have been tested for their effect on the GAT/GNase ratio of Ehrlich Ascites cells and host plasma. It was observed that all these drugs had changed the ratio of the 2 types of glutaminases from below 1.0 to the normal value of 1.0, this was accompanied with an increase in the survival time of the tumour-bearing animals. There was, however, no effect on the plasma GAT/GNase ratio of normal animals in the presence of the 3 antitumour compounds tested.     

Two new short-acting non-depolarizing neuromuscular blocking agents

Résumé Le chlorure de 1,1-octaméthylène et le méthylsulfate de 5,5-octaméthylènebis ont chez le chat un effet de blocage neuro-musculaire non dépolarisant, de courte durée. Les comparaisons faites avec des analogues voisins suggèrent que l'activité de ces composés est influencée par le degré d'empêchement stérique autour des atomes d'azote quaternaire. Les composés inhibent les acétylcholinestérases et s'opposent à des degrés divers aux effects muscariniques de l'acétylcholine.     

Diaryl pyrroles: A new series of anti-inflammatory agents

Zusammenfassung Die antiinflammatorischen Eigenschaften von verschiedenen Diaryl-pyrrol-Derivaten wurden untersucht. Es wurde festgestellt, dass eine repräsentative Verbindung, 2-Methyl-4, 5-bis(p-metoxyphenyl)-pyrrol, eine ausgeprägte Hemmung gegen das akute Ödem und die chronische Arthritis der Ratte zeigt.

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We thank Messrs.K. Wachi, Y. Umemuro andT. Kojima for their technical assistance.     

In vitro effects of melanocytolytic agents and other compounds upon dominant human melanoma tyrosinase activity

Summary The activity of dominant human melanoma tyrosinase isozyme was greatly decreased by certain reducing agents. The number and geometry of phenolic groups as well as free-SH group appear important for enzymic inhibition.This investigation was supported by U.S. Public Health Service Research Grant No. CA-12731-02 and CA-15991-01 from National Cancer Institute.     

Acylfulvenes,a new class of potent antitumor agents

Acylfulvene, derived from the sesquiterpene illudin S by treatment with acid (reverse Prins reaction), is far less reactive to thiols than illudin S. However, it is reduced readily to an aromatic product, in the same way as illudin S. This may explain its greatly improved therapeutic index compared to that of the parent compound.Unfortunately, publication was held up due to postal delay.     

Methylhydrazine derivatives,a new class of cytotoxic agents

Zusammenfassung Ausgehend von der Beobachtung, dass 1-Methyl-2-benzyl-hydrazin tumorhemmend wirkt, wurden durch systematische Variationen die für diese Wirkung essentiellen Strukturmerkmale festgelegt. Aus einer grösseren Anzahl von Verbindungen wurden 1-Methyl-2-p-(isopropylcarbamoyl)benzyl-hydrazin-hydrochlorid und 1-Methyl-2-p-allophanoylbenzyl-hydrazin-hydrobromid für ausgedehnte experimentelle und klinische Versuche ausgewählt.     

In vitro effects of melanocytolytic agents and other compounds upon dominant human melanoma tyrosinase activity.

The activity of dominant human melanoma tyrosinase isozyme was greatly decreased by certain reducing agents. The number and geometry of phenolic groups as well as free--SH group appear important for enzymic inhibition.     

The in vitro effect of adrenergic agents and related compounds on triglyceride levels of guinea-pig lymphoid cells

Summary Isoproterenol, epinephrine and norepinephrine were highly potent in decreasing the triglyceride levels of the splenic lymphoid cells from guinea-pigs in vitro, while they were quite inert upon the inguinal lymph node cells.     

Histamine sensitizing activity of lentinan,an antitumour polysaccharide

Riassunto E dimostrato che lentinan, polisaccaride antineoplastic, è capace di aumentare la sensibitità del topo contro istamina. La presomministrazione di lentinan invece non aumenta l'attività del fattore istamina sensibilizzante dellaBordetella pertussis. Lentinan non induce linfocitose nel topo.

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Acknowledgment: Thanks are due to Drs.G. Chihara andY. Y. Maeda, National Cancer Centre, Research Institute, Tokyo, for kindly supplying lentinan.     

The in vitro effect of adrenergic agents and related compounds on triglyceride levels of guinea-pig lymphoid cells.

Isoproterenol, epinephrine and norepinephrine were highly potent in decreasing the triglyceride levels of the splenic lymphoid cells from guinea-pigs in vitro, while they were quite inert upon the inguinal lymph node cells.