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A Novel Class of N-Sulfonyl and N-Sulfamoyl Noscapine Derivatives that Promote Mitotic Arrest in Cancer Cells.
ChemMedChem ( IF 3.6 ) Pub Date : 2019-11-12 , DOI: 10.1002/cmdc.201900477 Cassandra Yong 1 , Shane M Devine 1 , Xuexin Gao 2 , Angelina Yan 2 , Richard Callaghan 2 , Ben Capuano 1 , Peter J Scammells 1
ChemMedChem ( IF 3.6 ) Pub Date : 2019-11-12 , DOI: 10.1002/cmdc.201900477 Cassandra Yong 1 , Shane M Devine 1 , Xuexin Gao 2 , Angelina Yan 2 , Richard Callaghan 2 , Ben Capuano 1 , Peter J Scammells 1
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Noscapine displays weak anticancer efficacy and numerous research efforts have attempted to generate more potent noscapine analogues. These modifications included the replacement of the N-methyl group in the 6'-position with a range of substituents, where N-ethylcarbamoyl substitution was observed to possess enhanced anticancer activity. Herein, we describe advances in this area, namely the synthesis and pharmacological evaluation of a series of N-sulfonyl and N-sulfamoyl noscapine derivatives. A number of these sulfonyl-containing noscapinoids demonstrated improved activities compared to noscapine. ((R)-5-((S)-4,5-Dimethoxy-1,3-dihydroisobenzofuran-1-yl)-4-methoxy-6-((1-methyl-1H-imidazol-4-yl)sulfonyl)-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinoline) (14 q) displayed sub-micromolar activities of 560, 980, 271 and 443 nM against MCF-7, PANC-1, MDA-MB-435 and SK-MEL-5 cells, respectively. This antiproliferative effect was also maintained against drug-resistant NCI/AdrRES cells despite high expression of the multidrug efflux pump, P-glycoprotein.
中文翻译：
新型一类N-磺酰基和N-氨磺酰基Noscapine衍生物，可促进癌细胞中的有丝分裂。
Noscapine显示出较弱的抗癌功效，许多研究工作已尝试生成更有效的Noscapine类似物。这些修饰包括用一系列取代基取代6'-位的N-甲基，其中观察到N-乙基氨基甲酰基取代具有增强的抗癌活性。本文中，我们描述了该领域的进展，即一系列N-磺酰基和N-氨磺酰基Noscapine衍生物的合成和药理学评价。与Noscapine相比，许多这些含磺酰基的Noscapinoids表现出改善的活性。（（R）-5-（（S）-4,5-二甲氧基-1,3-二氢异苯并呋喃-1-基）-4-甲氧基-6-（（1-甲基-1H-咪唑-4-基）磺酰基）-5,6,7,8-四氢[1,3] dioxolo [4,5-g]异喹啉）（14 q）表现出对MCF-7的560、980、271和443 nM亚微摩尔活性，分别为PANC-1，MDA-MB-435和SK-MEL-5电池。尽管多药外排泵P-糖蛋白高表达，但这种抗增殖作用仍可抵抗耐药的NCI / AdrRES细胞。
更新日期：2019-11-13
中文翻译：
新型一类N-磺酰基和N-氨磺酰基Noscapine衍生物，可促进癌细胞中的有丝分裂。
Noscapine显示出较弱的抗癌功效，许多研究工作已尝试生成更有效的Noscapine类似物。这些修饰包括用一系列取代基取代6'-位的N-甲基，其中观察到N-乙基氨基甲酰基取代具有增强的抗癌活性。本文中，我们描述了该领域的进展，即一系列N-磺酰基和N-氨磺酰基Noscapine衍生物的合成和药理学评价。与Noscapine相比，许多这些含磺酰基的Noscapinoids表现出改善的活性。（（R）-5-（（S）-4,5-二甲氧基-1,3-二氢异苯并呋喃-1-基）-4-甲氧基-6-（（1-甲基-1H-咪唑-4-基）磺酰基）-5,6,7,8-四氢[1,3] dioxolo [4,5-g]异喹啉）（14 q）表现出对MCF-7的560、980、271和443 nM亚微摩尔活性，分别为PANC-1，MDA-MB-435和SK-MEL-5电池。尽管多药外排泵P-糖蛋白高表达，但这种抗增殖作用仍可抵抗耐药的NCI / AdrRES细胞。
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