苯乙基异硫氰酸酯(Phenethyl Isothiocyanate) - 药物靶点：HSF1 x Nrf2_在研适应症：前列腺增生症，肺癌，晚期前列腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Abrassin

靶点

HSF1 x Nrf2

作用方式

抑制剂、刺激剂

作用机制

HSF1抑制剂(heat shock transcription factor 1 inhibitors)、Nrf2刺激剂(核转录因子的激活红细胞2相关因子刺激剂)

治疗领域

肿瘤呼吸系统疾病泌尿生殖系统疾病

在研适应症

前列腺增生症肺癌晚期前列腺癌+ [1]

非在研适应症

烟草依赖

原研机构

University of Minnesota

在研机构

无锡杰西医药股份有限公司

非在研机构

University of Minnesota

权益机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)临床2期

特殊审评-

登录后查看时间轴

结构/序列

分子式C9H9NS

InChIKeyIZJDOKYDEWTZSO-UHFFFAOYSA-N

CAS号2257-09-2

关联

5

项与苯乙基异硫氰酸酯相关的临床试验

NCT00005883

/ Completed临床1期IIT

A Phase I - Part B Multiple Dose Trial of Phenethyl Isothiocyanate

RATIONALE: Chemoprevention therapy is the use of certain drugs to try to prevent the development or recurrence of cancer. Phenethyl isothiocyanate may be effective in preventing lung cancer in smokers.
PURPOSE: Phase I trial of phenethyl isothiocyanate in preventing lung cancer in people who smoke.

开始日期-

申办/合作机构

NYU Langone Health

[+1]

CTR20232507

/ Recruiting临床1期

JC-5411-L 在晚期实体瘤患者中的安全性、耐受性、药代动力学及初步疗效的多中心、开放Ⅰb/Ⅱ 期临床研究

主要研究目的： Ⅰb期：评价JC-5411-L在晚期实体瘤患者的安全性和耐受性，探索JC-5411-L的最大耐受剂量（MTD），确定II期临床研究推荐剂量（RP2D）。 Ⅱ期：评价JC-5411-L在卵巢癌患者中的有效性和安全性。次要研究目的：评价JC-5411-L的药代动力学（PK）特征。初步评价JC-5411-L治疗晚期实体瘤患者的疗效。探索性研究目的评价晚期实体瘤患者的肿瘤标本或外周血中的生物标记物水平（包括但不限于p53 蛋白表达水平）与疗效的关系。评价晚期实体瘤患者的GST基因型与疗效的关系。

开始日期2023-12-13

申办/合作机构

无锡杰西医药股份有限公司

NCT00691132

/ Completed临床2期IIT

Randomized Trial of PEITC as a Modifier of NNK Metabolism in Smokers

RATIONALE: Chemoprevention is the use of certain drugs to keep cancer from forming. The use of phenethyl isothiocyanate may prevent lung cancer in people who smoke cigarettes.
PURPOSE: This randomized clinical trial is studying phenethyl isothiocyanate to see how well it works in preventing lung cancer in smokers.

开始日期2009-02-01

申办/合作机构

University of Minnesota

[+1]

100 项与苯乙基异硫氰酸酯相关的临床结果

登录后查看更多信息

100 项与苯乙基异硫氰酸酯相关的转化医学

登录后查看更多信息

100 项与苯乙基异硫氰酸酯相关的专利（医药）

登录后查看更多信息

1,851

项与苯乙基异硫氰酸酯相关的文献（医药）

2025-12-01·Natural Products and Bioprospecting

Natural anticancer agents: prospection of medicinal and aromatic plants in modern chemoprevention and chemotherapy

Review

作者: Olivero-Verbel, Jesus ; Caballero-Gallardo, Karina ; Quintero-Rincón, Patricia

AbstractNatural products obtained from medicinal and aromatic plants are increasingly recognized as promising anticancer agents due to their structural richness, including terpene and flavonoid molecules, which induce apoptosis and modulate gene expression. These compounds offer an alternative to conventional treatments, often costly, which face challenges such as multidrug resistance. This review aims to provide a promising alternative approach to effectively control cancer by consolidating significant findings in identifying natural products and anticancer agent development from medicinal and aromatic plants. It synthesizes the findings of a comprehensive search of academic databases, such as PubMed and Springer, prioritizing articles published in recognized peer-reviewed journals that address the bioprospecting of medicinal and aromatic plants as anticancer agents. The review addresses the anticancer activities of plant extracts and essential oils, which were selected for their relevance to chemoprevention and chemotherapy. Compounds successfully used in cancer therapy include Docetaxel (an antimitotic agent), Etoposide VP-16 (an antimitotic agent and topoisomerase II inhibitor), Topotecan (a topoisomerase I inhibitor), Thymoquinone (a Reactive Oxygen Species-ROS inducer), and Phenethyl isothiocyanate (with multiple mechanisms). The review highlights natural products such as Hinokitiol, Mahanine, Hesperetin, Borneol, Carvacrol, Eugenol, Epigallocatechin gallate, and Capsaicin for their demonstrated efficacy against multiple cancer types, including breast, cervical, gastric, colorectal, pancreatic, lung, prostate, and skin cancer. Finally, it highlights the need for continued bioprospecting studies to identify novel natural products that can be successfully used in modern chemoprevention and chemotherapy.Graphical Abstract

2025-04-01·Bioorganic Chemistry

Novel carbazole-thiadiazole derivatives as α-amylase and α-glucosidase inhibitors: Design, biological evaluation, and computational insights

Article

作者: Jaradat, Nidal ; Hawash, Mohammed ; Çapan, İrfan ; Qaoud, Mohammed T

Diabetes mellitus remains a global health challenge, demanding innovative therapeutic solutions. Herein, we present the design, synthesis, and pharmacological evaluation of a novel series of carbazole-thiadiazole hybrids targeting key enzymes in carbohydrate metabolism. Among the synthesized compounds, 5l emerged as the most potent inhibitor of α-amylase, with an IC₅₀ value of 0.68 µM-far surpassing the efficacy of the standard drug acarbose (IC₅₀: 5.19 µM). Similarly, 5r exhibited exceptional dual activity against both α-amylase and α-glucosidase, with IC₅₀ values of 1.63 µM and 0.14 µM, respectively, highlighting its dual inhibitory potential. Biological assays demonstrated the compounds' low cytotoxicity on hepatic stellate (LX-2) cells, affirming their safety for therapeutic use. Molecular docking studies provided mechanistic insights into their binding interactions, revealing strong hydrogen bonding and hydrophobic interactions with key active site residues. Density functional theory (DFT) and electrostatic potential (ESP) analyses further elucidated their electronic properties, offering a deeper understanding of their structure-activity relationships. Pharmacokinetic profiling via the BOILED-Egg model confirmed these derivatives' excellent oral bioavailability and drug-likeness. Collectively, these findings establish carbazole-thiadiazole hybrids as promising candidates for next-generation antidiabetic therapies, warranting further investigation in preclinical and clinical settings.

2025-04-01·Bioorganic & Medicinal Chemistry

Development of carbazole-based molecules for inhibition of mutant hSOD1 protein aggregation in Amyotrophic Lateral Sclerosis

Article

作者: Sharma, Meenakshi ; Yadav, Kajal ; Mishra, Chandra Bhushan ; Gusain, Siddharth ; Saluja, Daman ; Tiwari, Manisha

Amyotrophic lateral sclerosis (ALS) is a neurodegenerative disease characterised by the loss of upper and lower motor neurons. Cu/Zn superoxide dismutase (SOD1) is one of the genes associated with the familial form of the disease (fALS). The mechanism of neuron degeneration by SOD1 is not clear, it is hypothesised that there is a toxic gain of function in the protein which leads to the downstream effects. In the present study, carbazole-based molecules have been rationally designed and synthesised as potential inhibitors of mutant hSOD1 protein aggregation. SG-9 and SG-10 prevented the aggregation of all three purified mutant hSOD1 proteins. Transmission electron microscopy and dynamic light scattering experiments also revealed that co-incubation of SG-9 and SG-10 with mutant hSOD1 protein resulted in smaller and slender fibril forming. Molecules SG-9 and SG-10 did not display toxicity and prevented Neuro-2a cells expressing hSOD1 G85R protein from its associated cytotoxicity. SG-9 and SG-10 were also able to prevent the transfected cells from apoptosis and were also able to reduce ROS levels associated with hSOD1 G85R protein aggregation significantly. Therefore, novel carbazole derivatives SG-9 and SG-10 proved to be effective inhibitors of mutant hSOD1 protein aggregation and can be further utilised as lead molecules for the amelioration of mutant hSOD1 aggregation-associated ALS.

100 项与苯乙基异硫氰酸酯相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
-	苯乙基异硫氰酸酯	-	DB12695

研发状态

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
晚期前列腺癌	临床2期	中国	无锡杰西医药股份有限公司	2021-12-15
前列腺增生症	临床2期	中国	无锡杰西医药股份有限公司	2014-04-04
肺癌	临床2期	-	无锡杰西医药股份有限公司	-
晚期恶性实体瘤	临床1期	中国	无锡杰西医药股份有限公司	2023-12-13
烟草依赖	临床前	美国	University of Minnesota	2009-02-01

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


AACR2011	N/A	乳腺癌	-	Phenethyl isothiocyanate (PEITC)	鹽壓鹹鹹襯醖膚顧顧憲(鑰範蓋鹹衊鹽衊範鬱繭) = 蓋廠積範鑰廠網繭衊鏇遞構製獵糧鑰糧製積憲 (窪蓋淵憲製廠鹽醖壓餘 )	-	2011-04-15