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首页> 外文期刊>Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry >Synthesis, Characterization and Pharmacological Evaluation of Some New 1,4-Diazepine Derivatives as Anticancer agents.
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Synthesis, Characterization and Pharmacological Evaluation of Some New 1,4-Diazepine Derivatives as Anticancer agents.

机译：一些新的1,4-二氮杂猪衍生物作为抗癌剂的合成，表征和药理评价。

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The new research work deals with the synthesis of cyclohepta[b]thieno[2,3-e][1,4]diazepine derivatives through three synthetic pathways starting with cycloheptanone. The starting ethyl 2-amino-5,6,7,8-tetrahydro-4Hcyclohepta[ b]thiophene-3-carboxylate (2) and 2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b] thiophene-3- carboxamide (5) was synthesized adopting a direct Gewald's method. The starting material 2 was reacted with phenacyl bromide and its chloride derivative to afford 3 a&b which further cyclized through the reaction with different aromatic amines to give 4a-e. Also 3-aryl-7,8,9,10-tetrahydro-1H,6H-cyclohepta[b]thieno[2,3-e][1,4] diazepin-5(4-H)-one (7a-f) was furnished via cyclization of 6 with phenacyl bromides. In addition, the reaction of the same starting material 6 with chloroacetyl chloride afforded 9 through the separated intermediate 8. All of the newly synthesized products were subjected to in vitro anticancer screening against human breast cancer cell line (MCF-7), colon cancer cell line (HCT-116) and against human liver carcinoma (HepG-2). Compounds 7 c, 7 e and 7 f were the most active compounds which exhibited antitumor activity against human hepatocellular carcinoma (HepG-2), human breast adenocarcinoma (MCF-7) and human colon carcinoma (HCT-116) cell lines, with IC50’s ranging from 4.4-13 μg/mL in a comparison to slandered vinblastine.
机译：新的研究工作涉及通过以环庚酮开始的三种合成途径合成Cycloppe [b]噻吩[2,3-e] [1,4]二氮杂肠衍生物。起始乙基2-氨基-5,6,7,8-四氢-4Hcyclohepta [B]噻吩-3-羧酸盐（2）和2-氨基-5,6,7,8-四氢-4H-环庚肽[B]合成噻吩-3-甲酰胺（5）采用直接的Gewald方法合成。原料2与苯溴化物及其氯化物衍生物反应，得到3 A＆B，其进一步通过与不同芳族胺的反应方式环化，得到4A-E。还有3-芳基-7,8,9,10-四氢-1H，6H-Cyclohepta [B] Thieno [2,3-e] [1,4]二氮杂化-5（4-H） - ONE（7A-F. ）通过用6用苯甲酸溴化物环化提供。此外，将相同的原料6与氯乙酰氯酰氯的反应得到9通过分离中间体8.所有新合成的产物都经受对人乳腺癌细胞系（MCF-7），结肠癌细胞的体外抗癌筛选线（HCT-116）和针对人肝癌（Hepg-2）。化合物7c，7 e和7f是最活跃的化合物，其表现出对人肝细胞癌（Hepg-2），人乳腺腺癌（MCF-7）和人结肠癌（HCT-116）细胞系的抗肿瘤活性，具有IC50与4.4-13μg/ ml相比，与诽谤压霉素相比。

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