一种铂 - 吖啶抗肿瘤药物的金（I）类似物仅具有中等细胞毒性，但对结核分枝杆菌显示出强效活性。
Gold(I) analogues of a platinum-acridine antitumor agent are only moderately cytotoxic but show potent activity against Mycobacterium tuberculosis.
作者信息
Eiter Lauren C, Hall Nathan W, Day Cynthia S, Saluta Gilda, Kucera Gregory L, Bierbach Ulrich
机构信息
Department of Chemistry, Wake Forest University, Winston-Salem, North Carolina 27109, USA.
出版信息
J Med Chem. 2009 Nov 12;52(21):6519-22. doi: 10.1021/jm9012856.
Abstract
Cationic gold(I) complexes containing 1-[2-(acridin-9-ylamino)ethyl]-1,3-dimethylthiourea (1), AuL(1) (where L is Cl(-), Br(-), SCN(-), PEt(3), PPh(3), or 1), derived from a class of analogous platinum(II) antitumor agents, have been synthesized. Unlike platinum, gold does not form permanent adducts with DNA, and its complexes are 2 orders of magnitude less cytotoxic in non-small-cell lung cancer cells than the most active platinum-based agent. Instead, several gold analogues show submicromolar and selective antimicrobial activity against Mycobacterium tuberculosis.
摘要
含有1-[2-(吖啶-9-基氨基)乙基]-1,3-二甲基硫脲(1)的阳离子金(I)配合物[AuL(1)](n +)(其中L为Cl(-)、Br(-)、SCN(-)、PEt(3)、PPh(3)或1)，是从一类类似的铂(II)抗肿瘤剂衍生而来的，已经被合成出来。与铂不同，金不会与DNA形成永久性加合物，并且其配合物在非小细胞肺癌细胞中的细胞毒性比活性最高的铂类药物低2个数量级。相反，几种金类似物对结核分枝杆菌表现出亚微摩尔级的选择性抗菌活性。
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