吲哚是平面雜環(huán)分子,對(duì)乳腺癌、肺癌、結(jié)腸癌等具有廣泛的抗癌活性,在藥物設(shè)計(jì)中發(fā)揮重要作用。從吲哚-3-甲醇及其代謝產(chǎn)物3,3′-二吲哚甲烷的結(jié)構(gòu)修飾、吲哚骨架結(jié)構(gòu)修飾、氧化吲哚衍生物及氮雜吲哚衍生物的結(jié)構(gòu)修飾入手,并綜合吲哚衍生物對(duì)Lumina型乳腺癌、三陰性乳腺癌、人表皮生長因子受體2(HER-2)過表達(dá)型乳腺癌的影響,從細(xì)胞水平、乳腺癌相關(guān)蛋白、受體、經(jīng)典通路、體內(nèi)外藥理模型建立以及相關(guān)指標(biāo)的變化等方面對(duì)其抗乳腺癌作用進(jìn)行系統(tǒng)綜述,以期為抗乳腺癌新藥研發(fā)提供依據(jù)。

Indole, a planar heterocyclic molecule, plays an important role in drug design due to its extensive anti-cancer activity against breast cancer, lung cancer and colon cancer. In this paper, the structure modification of indole-3-methanol(I3C) and its metabolite 3, 3'-diindolemethane(DIM), the structure modification of indole skeleton structure, the structure modification of oxidized indole derivatives and azaindole derivatives were studied. In addition, the effects of indole derivatives on Luminal type breast carcinoma, human epidermal growth factor receptor 2(HER-2) overexpression type breast carcinoma and triple negative breast cancer(TNBC) were summarized. The anti-breast cancer effects of indole derivatives were systematically reviewed from the aspects of cell level, breast cancer-related proteins, receptors, classical pathways, establishment of pharmacological models in vivo and in vitro, and changes of related indexes, to provide theoretical basis for the research of indole derivatives in the field of antibreast cancer drug innovation.

R285.5

天津市教育委員會(huì)重點(diǎn)項(xiàng)目(2022ZD041)