3,5-Bis(benzylidene)-1-(4-2-(morpholin-4-yl)ethoxyphenylcarbonyl)-4-piperidone hydrochloride: a lead tumor-specific cytotoxin which induces apoptosis and autophagy.

Das U; Sakagami H; Chu

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >3,5-Bis(benzylidene)-1-(4-2-(morpholin-4-yl)ethoxyphenylcarbonyl)-4-piperidone hydrochloride: a lead tumor-specific cytotoxin which induces apoptosis and autophagy.

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3,5-Bis(benzylidene)-1-(4-2-(morpholin-4-yl)ethoxyphenylcarbonyl)-4-piperidone hydrochloride: a lead tumor-specific cytotoxin which induces apoptosis and autophagy.

机译：3,5-双（亚苄基）-1-（4-2-（吗啉-4-基）乙氧基苯基羰基）-4-哌啶酮盐酸盐：一种主要的肿瘤特异性细胞毒素，可诱导细胞凋亡和自噬。

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A number of N-4-(2-aminoethoxy)phenylcarbonyl derivatives of various 3,5-bis(benzylidene)-4-piperidones 2-5 demonstrated noteworthy cytotoxic potencies towards human HL-60 leukemic cells as well as human HSC-2 and HSC-4 squamous cell carcinomas. In general, toxicity towards HGF, HPC, and HPLF normal cells was substantially lower. The highest selective toxicity was noted when the terminal base is morpholine. Lead optimization was based on finding compounds which had (i) high cytotoxic potencies, (ii) a greater toxicity to neoplasms than normal cells, and (iii) drug-likeness based on the rule of five. From the biodata generated, 5a evolved as a promising lead compound for further development. The mode of action of 5a included the induction of apoptosis in HL-60 cells in which internucleosomal DNA fragmentation and activation of caspase-3 was noted. In addition, 5a caused autophagy in HSC-2 cells.

机译：各种3,5-双（亚苄基）-4-哌啶酮2-5的许多N-4-（2-氨基乙氧基）苯基羰基衍生物对人HL-60白血病细胞以及人HSC-2和HSC-2具有显着的细胞毒性作用HSC-4鳞状细胞癌。通常，对HGF，HPC和HPLF正常细胞的毒性要低得多。当末端碱基为吗啉时，选择性毒性最高。铅优化基于发现具有以下特征的化合物：（i）具有比常规细胞更高的细胞毒性，（ii）对肿瘤更大的毒性，以及（iii）基于五律的药物相似性。从产生的生物数据来看，5a逐渐成为有前途的先导化合物，可以进一步开发。 5a的作用方式包括诱导HL-60细胞凋亡，其中注意到核小体间DNA片段化和caspase-3活化。另外，5a导致HSC-2细胞自噬。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第3期|共6页
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Das U; Sakagami H; Chu;
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1. 3,5-Bis(benzylidene)-1-(4-2-(morpholin-4-yl)ethoxyphenylcarbonyl)-4-piperidone hydrochloride: a lead tumor-specific cytotoxin which induces apoptosis and autophagy. [J] . Das U, Sakagami H, Chu Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：3,5-双（亚苄基）-1-（4-2-（吗啉-4-基）乙氧基苯基羰基）-4-哌啶酮盐酸盐：一种主要的肿瘤特异性细胞毒素，可诱导细胞凋亡和自噬。
2. CoMFA and CoMSIA studies on 1,3-Bis(benzylidene)-3,4-dihydro-1H-naphthalen-2-one, 2,6-bis(benzylidene)cyclohexanone, and 3,5-bis(benzylidene)-4-piperidone series of cytotoxic compounds [J] . Patel MR, Dimmock JR, Talele TT Journal of chemical information and modeling . 2007,第6期

机译：CoMFA和CoMSIA研究1,3-双（亚苄基）-3,4-二氢-1H-萘-2-酮，2,6-双（亚苄基）环己酮和3,5-双（亚苄基）-4-哌啶酮系列细胞毒性化合物
3. 1-[3-(2-Hydroxyethylsulfanyl)propanoyl]-3,5-bis(benzylidene)-4-piperidones: A novel cluster of P-glycoprotein dependent multidrug resistance modulators [J] . Das Umashankar, Pati Hari N., Barath Zoltan, Bioorganic and Medicinal Chemistry Letters . 2016,第4期

机译：1- [3-（2-羟乙基硫烷基）丙酰基] -3,5-双（亚苄基）-4-哌啶酮：一种新型的P-糖蛋白依赖性多药耐药性调节剂簇
4. 35-Bis(benzylidene)-1-4-2-(morpholin-4-yl)ethoxyphenylcarbonyl-4-piperidone hydrochloride: A lead tumor-specific cytotoxin which induces apoptosis and autophagy [O] . Umashankar Das, Hiroshi Sakagami, Qing Chu, -1

机译：35-双（苄基）-1- 4-2-（吗啉-4-基）乙氧基苯基羰基 -4-哌啶酮：盐酸铅肿瘤特异性细胞毒素其诱导细胞凋亡和自噬
5. 3,5-Bis(benzylidene)-1-4-2-(morpholin-4-yl)ethoxyphenylcarbonyl-4-piperidone hydrochloride: A lead tumor-specific cytotoxin which induces apoptosis and autophagy [O] . Umashankar Das, Hiroshi Sakagami, Qing Chu, 2010

机译：3,5-双（苄基）-1- 4-2-（吗啉-4-基）乙氧基苯基羰基 -4-哌啶酮：盐酸铅肿瘤特异性细胞毒素，其诱导细胞凋亡和自噬

3,5-Bis(benzylidene)-1-(4-2-(morpholin-4-yl)ethoxyphenylcarbonyl)-4-piperidone hydrochloride: a lead tumor-specific cytotoxin which induces apoptosis and autophagy.

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