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具有调节和控制上皮细胞正常生长、分化功能的维甲类,其特殊生理功能日益受到人们的重视,已被用于预防、治疗由化学致癌物等诱发的各种上皮肿瘤性病变的实验研究。并且,有些衍生物用于治疗人的癌前病变,如皮肤的老年性角化病、口腔、舌的白斑、膀胱乳头状瘤等均有一定的疗效。对人的皮肤基底细胞癌治疗,也有不同程度的缓解。但是,由于临床上的毒副作用,尽管维甲酸等抑癌效果很好,也难于广泛使用。因此,合成高效低毒的维甲酸衍生物成了当前药物合成化学研究的课题之
Retinoids, which regulate and control the normal growth and differentiation of epithelial cells, have attracted increasing attention for their special physiological functions. They have been used to prevent and treat various epithelial neoplastic lesions induced by chemical carcinogens. In addition, some derivatives are used to treat precancerous lesions in humans, such as senile keratoses of the skin, oral cavity, leukoplakia of the tongue, and papilloma of the bladder. There are also varying degrees of relief from treatment of human basal cell carcinoma of the skin. However, due to clinical toxicities and side effects, although antiretroviral drugs such as retinoic acid are effective, they are difficult to use widely. Therefore, the synthesis of highly effective and low-toxic retinoic acid derivatives has become the subject of current researches in the synthetic chemistry of pharmaceuticals.