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首页> 外文期刊>Medicinal chemistry >Synthesis and Anti-tumor Activities of Novel Phenyl Substituted Suberoylanilide Hydroxamic Acid Derivatives Against Human Cancer Cells
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Synthesis and Anti-tumor Activities of Novel Phenyl Substituted Suberoylanilide Hydroxamic Acid Derivatives Against Human Cancer Cells

机译：新型苯基取代的亚磺酰苯胺异羟肟酸衍生物的合成及其对人癌细胞的抗肿瘤活性

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摘要

A facile and atom-economical boric acid catalyzed direct amidation without any coupling agents for the preparation of Suberoylanilide Hydroxamic Acid (SAHA) and SAHA-based inhibitors targeting anti-proliferation of cancer cells is described. It is applicable to the preparation of SAHA-based inhibitors having an unprotected hydroxyl group in the phenyl ring without the need of the protection. The in-vitro assays data indicate that the nature and the position of the substituents (activating and/or deactivating) in the capping group (phenyl ring) of SAHA-based inhibitors synthesized in this study have a vital impact on the potency of anti-proliferative activity against cancer cells. With low toxicity toward the normal cells, a number of synthesized SAHA-based inhibitors with two substituents in the phenyl ring possess higher anti-proliferative activity than SAHA and Cisplatin toward six studied cancer cell lines: A375 human skin cancer cells, A549 human lung cancer cells, MGC80-3 human gastric cancer cells, H460 human lung cancer cells, H1299 human lung cancer cells, and HepG2 human liver cancer cells. Cisplatin is a common chemotherapeutic drug with high cytotoxicity for a variety of cancer treatments. The inhibitors provided in this study might signify future therapeutic drugs for cancer treatment.
机译：描述了一种容易的且原子经济的硼酸催化的直接酰胺化反应，无需任何偶联剂即可制备辛二酰苯胺异羟肟酸（SAHA）和针对癌细胞抗增殖的基于SAHA的抑制剂。它可用于制备在苯环中具有未保护的羟基而无需保护的SAHA基抑制剂。体外测定数据表明，在这项研究中合成的基于SAHA的抑制剂的封端基团（苯环）中取代基的性质和位置（活化和/或失活）对抗-脱氢酶的效力具有至关重要的影响。针对癌细胞的增殖活性。对正常细胞毒性低，许多合成的基于SAHA的苯环上具有两个取代基的抑制剂对SAH和顺铂对六种已研究的癌细胞系具有更高的抗增殖活性：A375人皮肤癌细胞，A549人肺癌细胞，MGC80-3人胃癌细胞，H460人肺癌细胞，H1299人肺癌细胞和HepG2人肝癌细胞。顺铂是一种常见的化学治疗药物，具有高细胞毒性，可用于多种癌症治疗。这项研究中提供的抑制剂可能表示未来用于癌症治疗的治疗药物。

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