Synthesis of Antitumor Antibiotics and their Model Compounds

亲癌素（CZ）和新抑癌素发色团（NCS-Chr）是已知的抗肿瘤抗生素，其结构尚未确定。我们预测cz与SS-Pharm，Co.，并通过合成它的左边部分来证实。为进行阿齐霉素的全合成，建立了有效的合成方法。针对NCS-Chr的体内抗肿瘤机制，我们采用新颖有效的方法合成了N-甲基吡咯寡聚体衍生物。研究了合成化合物在光照射下的DNA切割活性。为了寻找有效的抗肿瘤化合物，还合成了其它杂环化合物如AK-毒素和噻二唑类化合物。合成化合物的生物活性测试正在进行中。

Carzinophilin (CZ) and Neocarzinostatin Chromophore (NCS-Chr) are well known antitumor antibiotics, the structures of which are still not established. We predicted that cz is the same compound as Azinomycin which has been isolated by the research group of SS-Pharm, Co., and confirmed that by the synthesis of its left moiety. For the total synthesis of CZ (Azinomycin), we established the effective synthetic methods. In relation to the in vivo antitumor mechanisms of NCS-Chr, we synthesized oligo-N-methyl pyrrole derivatives by use of novel and efficient method. The DNA-cleaving activity of synthetic compounds under photo irradiation was investigated. Other heterocyclic compounds such as AK-toxin and some thiadiazoles were synthesized in order to search effective antitumor compounds. The test of bioactivities of synthetic compounds is under progress.