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蒽环抗生素柔毛霉素(1)和阿霉素(2)是有效的和临床应用的抗肿瘤药。同样,与此类似的洋红霉素(3)在临床试验中认为也是很有希望的抗肿瘤药物。然而,由于它们的稀少及其与许多抗肿瘤药物相同的副作用,例如骨髓损伤、口炎、脱发、畸变现象,尤其对心脏的累积毒性,因此限制了在化疗中广泛的使用。这些不希望的副作用促使人们继续对其同系物的研究,而这些合成的同系物(4～9)比母体药物显示更有利的治疗特性。本文报道了7-O-(2,6-二去氧-α-L-来苏一吡喃已糖基)柔毛霉素酮的合成。糖结构被认为对这类抗肿瘤药物的药理性质具有决定性的影响。
Anthracyclines daunomycin (1) and doxorubicin (2) are potent and clinically useful antineoplastic agents. Similarly, the similar malaromycin (3) is also considered a promising antitumor drug in clinical trials. However, their widespread use in chemotherapy has been limited due to their scarcity and their same side effects as many anti-tumor drugs, such as bone marrow damage, stomatitis, hair loss, aberrations, and especially the cumulative toxicity of the heart. These unwanted side effects motivate continued research on their homologues, and these synthetic homologues (4-9) show more favorable therapeutic properties than the parent drug. This paper reports the synthesis of 7-O- (2,6-dideoxy-α-L-lyxopyranosylhexose) daunorubicin. Sugar structure is believed to have a decisive influence on the pharmacological properties of such antineoplastic agents.