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Discovery of Inhibitors of .

ACS medicinal chemistry letters

Wangtrakuldee P, Byrd MS, Campos CG, Henderson MW, Zhang Z, Clare M, Masoudi A, Myler PJ, Horn JR, Cotter PA, Hagen TJ.
PMID: 24376907
ACS Med Chem Lett. 2013 Jul 01;4(8). doi: 10.1021/ml400034m.

Evaluation of a series of MetAP inhibitors in an in vitro enzyme activity assay led to the first identification of potent molecules that show significant growth inhibition against Burkholderia pseudomallei. Nitroxoline analogs show excellent inhibition potency in the BpMetAP1...

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Wangtrakuldee P, Byrd MS, Campos CG, et al. Discovery of Inhibitors of . ACS Med Chem Lett. 2013;4(8)doi: 10.1021/ml400034m.
Wangtrakuldee, P., Byrd, M. S., Campos, C. G., Henderson, M. W., Zhang, Z., Clare, M., Masoudi, A., Myler, P. J., Horn, J. R., Cotter, P. A., & Hagen, T. J. (2013). Discovery of Inhibitors of . ACS medicinal chemistry letters, 4(8), . https://doi.org/10.1021/ml400034m
Wangtrakuldee, Phumvadee, et al. "Discovery of Inhibitors of ." ACS medicinal chemistry letters vol. 4,8 (2013). doi: https://doi.org/10.1021/ml400034m
Wangtrakuldee P, Byrd MS, Campos CG, Henderson MW, Zhang Z, Clare M, Masoudi A, Myler PJ, Horn JR, Cotter PA, Hagen TJ. Discovery of Inhibitors of . ACS Med Chem Lett. 2013 Jul 01;4(8). doi: 10.1021/ml400034m. PMID: 24376907; PMCID: PMC3871185.
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Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.

European journal of medicinal chemistry

Proschak A, Martinelli G, Frank D, Rotter MJ, Brunst S, Weizel L, Burgers LD, Fürst R, Proschak E, Sosič I, Gobec S, Wichelhaus TA.
PMID: 34865870
Eur J Med Chem. 2022 Jan 15;228:113975. doi: 10.1016/j.ejmech.2021.113975. Epub 2021 Nov 13.

Carbapenemases such as metallo-β-lactamases (MBLs) are spreading among Gram-negative bacterial pathogens. Infections due to these multidrug-resistant bacteria constitute a major global health challenge. Therapeutic strategies against carbapenemase producing bacteria include β-lactamase inhibitor combinations. Nitroxoline is a broad-spectrum antibiotic with...

Cite
Proschak A, Martinelli G, Frank D, et al. Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases. Eur J Med Chem. 2021;228:113975doi: 10.1016/j.ejmech.2021.113975.
Proschak, A., Martinelli, G., Frank, D., Rotter, M. J., Brunst, S., Weizel, L., Burgers, L. D., Fürst, R., Proschak, E., Sosič, I., Gobec, S., & Wichelhaus, T. A. (2022). Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases. European journal of medicinal chemistry, 228113975. https://doi.org/10.1016/j.ejmech.2021.113975
Proschak, Anna, et al. "Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases." European journal of medicinal chemistry vol. 228 (2022): 113975. doi: https://doi.org/10.1016/j.ejmech.2021.113975
Proschak A, Martinelli G, Frank D, Rotter MJ, Brunst S, Weizel L, Burgers LD, Fürst R, Proschak E, Sosič I, Gobec S, Wichelhaus TA. Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases. Eur J Med Chem. 2022 Jan 15;228:113975. doi: 10.1016/j.ejmech.2021.113975. Epub 2021 Nov 13. PMID: 34865870.
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Evaluation of Disulfiram Drug Combinations and Identification of Other More Effective Combinations against Stationary Phase .

Antibiotics (Basel, Switzerland)

Alvarez-Manzo HS, Zhang Y, Shi W, Zhang Y.
PMID: 32858987
Antibiotics (Basel). 2020 Aug 26;9(9). doi: 10.3390/antibiotics9090542.

Lyme disease, caused by

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Alvarez-Manzo HS, Zhang Y, Shi W, et al. Evaluation of Disulfiram Drug Combinations and Identification of Other More Effective Combinations against Stationary Phase . Antibiotics (Basel). 2020;9(9)doi: 10.3390/antibiotics9090542.
Alvarez-Manzo, H. S., Zhang, Y., Shi, W., & Zhang, Y. (2020). Evaluation of Disulfiram Drug Combinations and Identification of Other More Effective Combinations against Stationary Phase . Antibiotics (Basel, Switzerland), 9(9), . https://doi.org/10.3390/antibiotics9090542
Alvarez-Manzo, Hector S, et al. "Evaluation of Disulfiram Drug Combinations and Identification of Other More Effective Combinations against Stationary Phase ." Antibiotics (Basel, Switzerland) vol. 9,9 (2020). doi: https://doi.org/10.3390/antibiotics9090542
Alvarez-Manzo HS, Zhang Y, Shi W, Zhang Y. Evaluation of Disulfiram Drug Combinations and Identification of Other More Effective Combinations against Stationary Phase . Antibiotics (Basel). 2020 Aug 26;9(9). doi: 10.3390/antibiotics9090542. PMID: 32858987; PMCID: PMC7559458.
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Derivatives (halogen, nitro and amino) of 8-hydroxyquinoline with highly potent antimicrobial and antioxidant activities.

Biochemistry and biophysics reports

Cherdtrakulkiat R, Boonpangrak S, Sinthupoom N, Prachayasittikul S, Ruchirawat S, Prachayasittikul V.
PMID: 29214226
Biochem Biophys Rep. 2016 Mar 24;6:135-141. doi: 10.1016/j.bbrep.2016.03.014. eCollection 2016 Jul.

8-Hydroxyquinoline (8HQ) compounds have been reported to possess diverse bioactivities. In recent years, drug repositioning has gained considerable attention in drug discovery and development. Herein, 8HQ (

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Cherdtrakulkiat R, Boonpangrak S, Sinthupoom N, et al. Derivatives (halogen, nitro and amino) of 8-hydroxyquinoline with highly potent antimicrobial and antioxidant activities. Biochem Biophys Rep. 2016;6:135-141doi: 10.1016/j.bbrep.2016.03.014.
Cherdtrakulkiat, R., Boonpangrak, S., Sinthupoom, N., Prachayasittikul, S., Ruchirawat, S., & Prachayasittikul, V. (2016). Derivatives (halogen, nitro and amino) of 8-hydroxyquinoline with highly potent antimicrobial and antioxidant activities. Biochemistry and biophysics reports, 6135-141. https://doi.org/10.1016/j.bbrep.2016.03.014
Cherdtrakulkiat, Rungrot, et al. "Derivatives (halogen, nitro and amino) of 8-hydroxyquinoline with highly potent antimicrobial and antioxidant activities." Biochemistry and biophysics reports vol. 6 (2016): 135-141. doi: https://doi.org/10.1016/j.bbrep.2016.03.014
Cherdtrakulkiat R, Boonpangrak S, Sinthupoom N, Prachayasittikul S, Ruchirawat S, Prachayasittikul V. Derivatives (halogen, nitro and amino) of 8-hydroxyquinoline with highly potent antimicrobial and antioxidant activities. Biochem Biophys Rep. 2016 Mar 24;6:135-141. doi: 10.1016/j.bbrep.2016.03.014. eCollection 2016 Jul. PMID: 29214226; PMCID: PMC5689172.
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Effect of 8-hydroxyquinoline and derivatives on human neuroblastoma SH-SY5Y cells under high glucose.

PeerJ

Suwanjang W, Prachayasittikul S, Prachayasittikul V.
PMID: 27635352
PeerJ. 2016 Aug 31;4:e2389. doi: 10.7717/peerj.2389. eCollection 2016.

8-Hydroxyquinoline and derivatives exhibit multifunctional properties, including antioxidant, antineurodegenerative, anticancer, anti-inflammatory and antidiabetic activities. In biological systems, elevation of intracellular calcium can cause calpain activation, leading to cell death. Here, the effect of 8-hydroxyquinoline and derivatives (5-chloro-7-iodo-8-hydroxyquinoline or clioquinol...

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Suwanjang W, Prachayasittikul S, Prachayasittikul V. Effect of 8-hydroxyquinoline and derivatives on human neuroblastoma SH-SY5Y cells under high glucose. PeerJ. 2016;4:e2389doi: 10.7717/peerj.2389.
Suwanjang, W., Prachayasittikul, S., & Prachayasittikul, V. (2016). Effect of 8-hydroxyquinoline and derivatives on human neuroblastoma SH-SY5Y cells under high glucose. PeerJ, 4e2389. https://doi.org/10.7717/peerj.2389
Suwanjang, Wilasinee, et al. "Effect of 8-hydroxyquinoline and derivatives on human neuroblastoma SH-SY5Y cells under high glucose." PeerJ vol. 4 (2016): e2389. doi: https://doi.org/10.7717/peerj.2389
Suwanjang W, Prachayasittikul S, Prachayasittikul V. Effect of 8-hydroxyquinoline and derivatives on human neuroblastoma SH-SY5Y cells under high glucose. PeerJ. 2016 Aug 31;4:e2389. doi: 10.7717/peerj.2389. eCollection 2016. PMID: 27635352; PMCID: PMC5012261.
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Discovery and Validation of Nitroxoline as a Novel STAT3 Inhibitor in Drug-resistant Urothelial Bladder Cancer.

International journal of biological sciences

Lin W, Sun J, Sadahira T, Xu N, Wada K, Liu C, Araki M, Xu A, Watanabe M, Nasu Y, Huang P.
PMID: 34421363
Int J Biol Sci. 2021 Jul 25;17(12):3255-3267. doi: 10.7150/ijbs.63125. eCollection 2021.

Repeated cycles of first-line chemotherapy drugs such as doxorubicin (DOX) and cisplatin (CIS) trigger frequent chemoresistance in recurrent urothelial bladder cancer (UBC). Nitroxoline (NTX), an antibiotic to treat urinary tract infections, has been recently repurposed for cancer treatment. Here...

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Lin W, Sun J, Sadahira T, et al. Discovery and Validation of Nitroxoline as a Novel STAT3 Inhibitor in Drug-resistant Urothelial Bladder Cancer. Int J Biol Sci. 2021;17(12):3255-3267doi: 10.7150/ijbs.63125.
Lin, W., Sun, J., Sadahira, T., Xu, N., Wada, K., Liu, C., Araki, M., Xu, A., Watanabe, M., Nasu, Y., & Huang, P. (2021). Discovery and Validation of Nitroxoline as a Novel STAT3 Inhibitor in Drug-resistant Urothelial Bladder Cancer. International journal of biological sciences, 17(12), 3255-3267. https://doi.org/10.7150/ijbs.63125
Lin, Wenfeng, et al. "Discovery and Validation of Nitroxoline as a Novel STAT3 Inhibitor in Drug-resistant Urothelial Bladder Cancer." International journal of biological sciences vol. 17,12 (2021): 3255-3267. doi: https://doi.org/10.7150/ijbs.63125
Lin W, Sun J, Sadahira T, Xu N, Wada K, Liu C, Araki M, Xu A, Watanabe M, Nasu Y, Huang P. Discovery and Validation of Nitroxoline as a Novel STAT3 Inhibitor in Drug-resistant Urothelial Bladder Cancer. Int J Biol Sci. 2021 Jul 25;17(12):3255-3267. doi: 10.7150/ijbs.63125. eCollection 2021. PMID: 34421363; PMCID: PMC8375225.
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TRIM25 activates AKT/mTOR by inhibiting PTEN via K63-linked polyubiquitination in non-small cell lung cancer.

Acta pharmacologica Sinica

He YM, Zhou XM, Jiang SY, Zhang ZB, Cao BY, Liu JB, Zeng YY, Zhao J, Mao XL.
PMID: 33931764
Acta Pharmacol Sin. 2021 Apr 30; doi: 10.1038/s41401-021-00662-z. Epub 2021 Apr 30.

The PTEN/AKT/mTOR signaling pathway is frequently dysregulated in non-small cell lung cancer (NSCLC), but the mechanisms are not well-understood. The present study found that the ubiquitin ligase TRIM25 is highly expressed in NSCLC tissues and promotes NSCLC cell survival...

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He YM, Zhou XM, Jiang SY, et al. TRIM25 activates AKT/mTOR by inhibiting PTEN via K63-linked polyubiquitination in non-small cell lung cancer. Acta Pharmacol Sin. 2021;doi: 10.1038/s41401-021-00662-z.
He, Y. M., Zhou, X. M., Jiang, S. Y., Zhang, Z. B., Cao, B. Y., Liu, J. B., Zeng, Y. Y., Zhao, J., & Mao, X. L. (2021). TRIM25 activates AKT/mTOR by inhibiting PTEN via K63-linked polyubiquitination in non-small cell lung cancer. Acta pharmacologica Sinica, . https://doi.org/10.1038/s41401-021-00662-z
He, Yuan-Ming, et al. "TRIM25 activates AKT/mTOR by inhibiting PTEN via K63-linked polyubiquitination in non-small cell lung cancer." Acta pharmacologica Sinica vol. (2021). doi: https://doi.org/10.1038/s41401-021-00662-z
He YM, Zhou XM, Jiang SY, Zhang ZB, Cao BY, Liu JB, Zeng YY, Zhao J, Mao XL. TRIM25 activates AKT/mTOR by inhibiting PTEN via K63-linked polyubiquitination in non-small cell lung cancer. Acta Pharmacol Sin. 2021 Apr 30; doi: 10.1038/s41401-021-00662-z. Epub 2021 Apr 30. PMID: 33931764.
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Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.

European journal of medicinal chemistry

Proschak A, Martinelli G, Frank D, Rotter MJ, Brunst S, Weizel L, Burgers LD, Fürst R, Proschak E, Sosič I, Gobec S, Wichelhaus TA.
PMID: 34865870
Eur J Med Chem. 2022 Jan 15;228:113975. doi: 10.1016/j.ejmech.2021.113975. Epub 2021 Nov 13.

Carbapenemases such as metallo-β-lactamases (MBLs) are spreading among Gram-negative bacterial pathogens. Infections due to these multidrug-resistant bacteria constitute a major global health challenge. Therapeutic strategies against carbapenemase producing bacteria include β-lactamase inhibitor combinations. Nitroxoline is a broad-spectrum antibiotic with...

Cite
Proschak A, Martinelli G, Frank D, et al. Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases. Eur J Med Chem. 2021;228:113975doi: 10.1016/j.ejmech.2021.113975.
Proschak, A., Martinelli, G., Frank, D., Rotter, M. J., Brunst, S., Weizel, L., Burgers, L. D., Fürst, R., Proschak, E., Sosič, I., Gobec, S., & Wichelhaus, T. A. (2022). Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases. European journal of medicinal chemistry, 228113975. https://doi.org/10.1016/j.ejmech.2021.113975
Proschak, Anna, et al. "Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases." European journal of medicinal chemistry vol. 228 (2022): 113975. doi: https://doi.org/10.1016/j.ejmech.2021.113975
Proschak A, Martinelli G, Frank D, Rotter MJ, Brunst S, Weizel L, Burgers LD, Fürst R, Proschak E, Sosič I, Gobec S, Wichelhaus TA. Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases. Eur J Med Chem. 2022 Jan 15;228:113975. doi: 10.1016/j.ejmech.2021.113975. Epub 2021 Nov 13. PMID: 34865870.
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Repurposing of 8-Hydroxyquinoline-based Butyrylcholinesterase and Cathepsin B Ligands as Potent Non-peptidic Deoxyribonuclease I Inhibitors.

ChemMedChem

Gajic M, Knez D, Sosič I, Mravljak J, Meden A, Košak U, Leitzbach L, George S, Hofmann B, Zivkovic A, Steinhilber D, Stark H, Gobec S, Smelcerovic A, Anderluh M.
PMID: 34994078
ChemMedChem. 2022 Jan 07; doi: 10.1002/cmdc.202100694. Epub 2022 Jan 07.

A library of 31 butyrylcholinesterase (BChE) and cathepsin B (CatB) inhibitors, was screened in vitro for inhibition of deoxyribonuclease I (DNase I). Compounds 22, 8 and 7 are among the most potent synthetic non-peptide DNase I inhibitors reported up...

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Gajic M, Knez D, Sosič I, et al. Repurposing of 8-Hydroxyquinoline-based Butyrylcholinesterase and Cathepsin B Ligands as Potent Non-peptidic Deoxyribonuclease I Inhibitors. ChemMedChem. 2022;doi: 10.1002/cmdc.202100694.
Gajic, M., Knez, D., Sosič, I., Mravljak, J., Meden, A., Košak, U., Leitzbach, L., George, S., Hofmann, B., Zivkovic, A., Steinhilber, D., Stark, H., Gobec, S., Smelcerovic, A., & Anderluh, M. (2022). Repurposing of 8-Hydroxyquinoline-based Butyrylcholinesterase and Cathepsin B Ligands as Potent Non-peptidic Deoxyribonuclease I Inhibitors. ChemMedChem, . https://doi.org/10.1002/cmdc.202100694
Gajic, Mihajlo, et al. "Repurposing of 8-Hydroxyquinoline-based Butyrylcholinesterase and Cathepsin B Ligands as Potent Non-peptidic Deoxyribonuclease I Inhibitors." ChemMedChem vol. (2022). doi: https://doi.org/10.1002/cmdc.202100694
Gajic M, Knez D, Sosič I, Mravljak J, Meden A, Košak U, Leitzbach L, George S, Hofmann B, Zivkovic A, Steinhilber D, Stark H, Gobec S, Smelcerovic A, Anderluh M. Repurposing of 8-Hydroxyquinoline-based Butyrylcholinesterase and Cathepsin B Ligands as Potent Non-peptidic Deoxyribonuclease I Inhibitors. ChemMedChem. 2022 Jan 07; doi: 10.1002/cmdc.202100694. Epub 2022 Jan 07. PMID: 34994078.
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Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.

European journal of medicinal chemistry

Proschak A, Martinelli G, Frank D, Rotter MJ, Brunst S, Weizel L, Burgers LD, Fürst R, Proschak E, Sosič I, Gobec S, Wichelhaus TA.
PMID: 34865870
Eur J Med Chem. 2021 Nov 13;113975. doi: 10.1016/j.ejmech.2021.113975. Epub 2021 Nov 13.

Carbapenemases such as metallo-β-lactamases (MBLs) are spreading among Gram-negative bacterial pathogens. Infections due to these multidrug-resistant bacteria constitute a major global health challenge. Therapeutic strategies against carbapenemase producing bacteria include β-lactamase inhibitor combinations. Nitroxoline is a broad-spectrum antibiotic with...

Cite
Proschak A, Martinelli G, Frank D, et al. Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases. Eur J Med Chem. 2021;113975doi: 10.1016/j.ejmech.2021.113975.
Proschak, A., Martinelli, G., Frank, D., Rotter, M. J., Brunst, S., Weizel, L., Burgers, L. D., Fürst, R., Proschak, E., Sosič, I., Gobec, S., & Wichelhaus, T. A. (2021). Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases. European journal of medicinal chemistry, 113975. https://doi.org/10.1016/j.ejmech.2021.113975
Proschak, Anna, et al. "Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases." European journal of medicinal chemistry vol. (2021): 113975. doi: https://doi.org/10.1016/j.ejmech.2021.113975
Proschak A, Martinelli G, Frank D, Rotter MJ, Brunst S, Weizel L, Burgers LD, Fürst R, Proschak E, Sosič I, Gobec S, Wichelhaus TA. Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases. Eur J Med Chem. 2021 Nov 13;113975. doi: 10.1016/j.ejmech.2021.113975. Epub 2021 Nov 13. PMID: 34865870.
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Nitroxoline inhibits bladder cancer progression by reversing EMT process and enhancing anti-tumor immunity.

Journal of Cancer

Xu N, Lin W, Sun J, Sadahira T, Xu A, Watanabe M, Guo K, Araki M, Li G, Liu C, Nasu Y, Huang P.
PMID: 33046984
J Cancer. 2020 Sep 23;11(22):6633-6641. doi: 10.7150/jca.47025. eCollection 2020.

Nitroxoline is considered to be an effective treatment for the urinary tract infections. Recently, it has been found to be effective against several cancers. However, few studies have examined the anti-tumor activity of nitroxoline in bladder cancer. The purpose...

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Xu N, Lin W, Sun J, et al. Nitroxoline inhibits bladder cancer progression by reversing EMT process and enhancing anti-tumor immunity. J Cancer. 2020;11(22):6633-6641doi: 10.7150/jca.47025.
Xu, N., Lin, W., Sun, J., Sadahira, T., Xu, A., Watanabe, M., Guo, K., Araki, M., Li, G., Liu, C., Nasu, Y., & Huang, P. (2020). Nitroxoline inhibits bladder cancer progression by reversing EMT process and enhancing anti-tumor immunity. Journal of Cancer, 11(22), 6633-6641. https://doi.org/10.7150/jca.47025
Xu, Naijin, et al. "Nitroxoline inhibits bladder cancer progression by reversing EMT process and enhancing anti-tumor immunity." Journal of Cancer vol. 11,22 (2020): 6633-6641. doi: https://doi.org/10.7150/jca.47025
Xu N, Lin W, Sun J, Sadahira T, Xu A, Watanabe M, Guo K, Araki M, Li G, Liu C, Nasu Y, Huang P. Nitroxoline inhibits bladder cancer progression by reversing EMT process and enhancing anti-tumor immunity. J Cancer. 2020 Sep 23;11(22):6633-6641. doi: 10.7150/jca.47025. eCollection 2020. PMID: 33046984; PMCID: PMC7545671.
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Addition of 2-(ethylamino)acetonitrile group to nitroxoline results in significantly improved anti-tumor activity .

Oncotarget

Mitrović A, Sosič I, Kos Š, Tratar UL, Breznik B, Kranjc S, Mirković B, Gobec S, Lah T, Serša G, Kos J.
PMID: 28938624
Oncotarget. 2017 Jul 17;8(35):59136-59147. doi: 10.18632/oncotarget.19296. eCollection 2017 Aug 29.

Lysosomal cysteine peptidase cathepsin B, involved in multiple processes associated with tumor progression, is validated as a target for anti-cancer therapy. Nitroxoline, a known antimicrobial agent, is a potent and selective inhibitor of cathepsin B, hence reducing tumor progression

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Mitrović A, Sosič I, Kos Š, et al. Addition of 2-(ethylamino)acetonitrile group to nitroxoline results in significantly improved anti-tumor activity . Oncotarget. 2017;8(35):59136-59147doi: 10.18632/oncotarget.19296.
Mitrović, A., Sosič, I., Kos, �. �., Tratar, U. L., Breznik, B., Kranjc, S., Mirković, B., Gobec, S., Lah, T., Serša, G., & Kos, J. (2017). Addition of 2-(ethylamino)acetonitrile group to nitroxoline results in significantly improved anti-tumor activity . Oncotarget, 8(35), 59136-59147. https://doi.org/10.18632/oncotarget.19296
Mitrović, Ana, et al. "Addition of 2-(ethylamino)acetonitrile group to nitroxoline results in significantly improved anti-tumor activity ." Oncotarget vol. 8,35 (2017): 59136-59147. doi: https://doi.org/10.18632/oncotarget.19296
Mitrović A, Sosič I, Kos Š, Tratar UL, Breznik B, Kranjc S, Mirković B, Gobec S, Lah T, Serša G, Kos J. Addition of 2-(ethylamino)acetonitrile group to nitroxoline results in significantly improved anti-tumor activity . Oncotarget. 2017 Jul 17;8(35):59136-59147. doi: 10.18632/oncotarget.19296. eCollection 2017 Aug 29. PMID: 28938624; PMCID: PMC5601720.
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