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1- (2- (2- ((7- chloroquinolin- 4- yl)amino)ethyl- methylamino)ethylamino)- 4- methylthioxanthen- 9- one

hydroxychloroquine derivative that inhibits autophagy and has antineoplastic properties

Also Known As:

ROC-325

Networked: 5 relevant articles (2 outcomes, 2 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Quinolines: 146
      - Aminoquinolines: 29
        Chloroquine: 7498
        Hydroxychloroquine: 4560
        1-(2-(2-((7-chloroquinolin-4-yl)amino)ethyl-methylamino)ethylamino)-4-methylthioxanthen-9-one: 5

Experts

1.	Carew, Jennifer S: 2 articles (06/2017 - 04/2017)
2.	Nawrocki, Steffan T: 2 articles (06/2017 - 04/2017)
3.	Deng, Ju: 1 article (06/2021)
4.	Li, Zhen-Yu: 1 article (06/2021)
5.	Liu, Hui-Min: 1 article (06/2021)
6.	Shi, Meng-Ya: 1 article (06/2021)
7.	Yao, Yao: 1 article (06/2021)
8.	Yuan, Can-Li: 1 article (06/2021)
9.	Espitia, Claudia M: 1 article (06/2017)
10.	Han, Yingchun: 1 article (06/2017)

Related Diseases

1.	Renal Cell Carcinoma (Grawitz Tumor) 06/01/2017 - "Comprehensive in vitro and in vivo studies were conducted to evaluate the selectivity, tolerability, and efficacy of ROC-325 in preclinical models of renal cell carcinoma (RCC) with HCQ serving as a comparator. " 06/01/2017 - "Disruption of Autophagic Degradation with ROC-325 Antagonizes Renal Cell Carcinoma Pathogenesis." 04/03/2017 - "Detailed in vitro and in vivo studies in preclinical models of renal cell carcinoma demonstrated that ROC-325 triggered the hallmark features of lysosomal autophagy inhibition, was very well tolerated, and exhibited significant superiority with respect to autophagy inhibition and anticancer activity over hydroxychloroquine. "
2.	Neoplasms (Cancer) 04/03/2017 - "Our findings support the clinical investigation of the safety and preliminary efficacy of ROC-325 in patients with autophagy-dependent malignancies and other disorders where aberrant autophagy contributes to disease pathogenesis." 06/01/2017 - "Oral administration of ROC-325 to mice bearing 786-0 RCC xenografts was well tolerated, was significantly more effective at inhibiting tumor progression than HCQ, and inhibited autophagy in vivoConclusions: Our findings demonstrate that ROC-325 has superior preclinical anticancer activity compared with HCQ and support the clinical investigation of its safety and preliminary efficacy in patients with RCC and other autophagy-dependent malignancies. " 06/01/2017 - ": ROC-325 exhibited superior in vitro anticancer effects compared with the existing autophagy inhibitor hydroxychloroquine (HCQ) in 12 different cancer cell lines with diverse genetic backgrounds. "
3.	Vascular Remodeling 01/01/2023 - "Hemodynamics, echocardiography, and histology measurement showed that ROC-325 treatment prevented the development of PH, right ventricular hypertrophy, fibrosis, dysfunction, and vascular remodeling after monocrotaline and Sugen5416/hypoxia administration. "
4.	Right Ventricular Hypertrophy 01/01/2023 - "Hemodynamics, echocardiography, and histology measurement showed that ROC-325 treatment prevented the development of PH, right ventricular hypertrophy, fibrosis, dysfunction, and vascular remodeling after monocrotaline and Sugen5416/hypoxia administration. "
5.	Multiple Myeloma 06/01/2021 - "Multiple myeloma cells were treated with ROC-325 at different concentration. " 06/01/2021 - "[The Inhibiting Effect of Autophagy Inhibitor ROC-325 on Multiple Myeloma]." 06/01/2021 - "To investigate the effects of autophagy inhibitor ROC-325 and its combination with bortezomib on the proliferation, apoptosis and autophagy of multiple myeloma cell lines. "

Related Drugs and Biologics

1.	Hydroxychloroquine (Plaquenil)
2.	Nitric Oxide Synthase Type III (Endothelial Nitric Oxide Synthase)
3.	Monocrotaline
4.	Nitric Oxide (Nitrogen Monoxide)
5.	Bortezomib (Velcade)

Related Therapies and Procedures

1.	Oral Administration