Vergleich der biologischen Wirksamkeit von C‐ und N‐MANNICH‐Basen mit und ohne Stickstofflost‐Gruppen in mikrobiologischen und tierexperimentellen Screening‐Systemen zur Suche nach Cancerostatica

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Abstract
In order to detect specific inhibitors of DNA synthesis with potential cancerostatic properties from microbial or chemical sources, a complex screening program in vitro and in vivo has been developed. This screening program consists both of molecularbiological models and rodent transplanted tumor systems. The microbiological screening program has proved to be of value in the primary selection of 95 mostly new synthesized compounds belonging to the C‐ and N‐MANNICH bases with or without nitrogen mustard groups. All the compounds detected by this screening are potential inhibitors of DNA synthesis and, therefore, able to disturb selectively mechanisms operating both in microbial and mammalian cells, e. g., replication, transcription, recombination, excission, and integration of DNA. Positive results concerning the correlation between effectivity in vitro and in vivo antitumor activity using rodent transplanted tumor systems are presented. Since most of the present day, alkylating agents are selectively toxic for cells which actively synthesize DNA, it is not surprising that there is some degree of correlation between antitumor effect and effects on various microbial or other rapidly growing organisms. However, evidence that agents with prophage inducing capability in lysogenic bacteria and/or with activity in the “BIP” test might play a part in cancer chemotherapy is obvious. The selectivity of the microbiological screening models used shows that they are potential screens despite their inabilities, thus far, to detect all active cancerostatics.

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