Design, Synthesis, and Evaluation of Heat Shock Protein 90 Inhibitors in Human Breast Cancer and Its Metastasis

Gümüş, Mehmet; Özgür, Aykut; Tutar, Lütfi; Dişli, Ali; Koca, İrfan; Tutar, Yusuf

doi:10.2174/1389201017666161031105815

Cited by 21 publications

(9 citation statements)

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“…The mixture of compound 359 and ethyl 4‐chloro‐3‐oxobutanoate ( 360 ) reagent was refluxed in acetonitrile for 2 hours to synthesize thiazolyl‐β‐ketoester compounds ( 361 ). The importance of synthesis of thiazole compounds from enamines was especially emphasized for the chemistry of heterocyclic compounds by Koca et al [84,85] . (Scheme 47).…”

Section: Formation Of Heterocycle Structures By Dmf‐dma Reactionsmentioning

confidence: 99%

Enamines and Dimethylamino Imines as Building Blocks in Heterocyclic Synthesis: Reactions of DMF‐DMA Reagent with Different Functional Groups

Gümüş

Koca

2020

ChemistrySelect

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N,N‐Dimethylformamide dimethyl acetal (DMF‐DMA) reagent can react with different functional groups of organic compounds. Enamines and dimethylamino imines are obtained, when the DMF‐DMA reagent is reacted with methylene, methyl and amino groups. These products are formed in the intermediate step in the synthesis of many hetero rings. These compounds are especially used as a starting material in the synthesis of heterostructures such as pyrimidine, pyridine, pyrazole, etc. Therefore, DMF‐DMA has been particularly prominent as a reagent in targeted synthesis and designs of many heterocyclic compounds. Herein, the reactions of DMF‐DMA reagent with different functional groups are categorized in four classes (methylene, methyl, amino, other groups) and the reactions of obtained enamine and dimethylamino imine compounds are investigated in detail such as nucleophilic addition, intramolecular cyclization or condensation reactions. The synthesis and continuation reactions of the enamine and dimethylamino imine compounds are also examined in terms of experimental conditions and reagents used.

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Section: Formation Of Heterocycle Structures By Dmf‐dma Reactionsmentioning

confidence: 99%

Enamines and Dimethylamino Imines as Building Blocks in Heterocyclic Synthesis: Reactions of DMF‐DMA Reagent with Different Functional Groups

Gümüş

Koca

2020

ChemistrySelect

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“…The XTT test was used to quantify the number of viable cells in each of the well in different concentrations [15,16]. Initially, the cancer cells were seeded in sterile 96-well culture plate (10x10 4 cells in each well), and the different concentrations of gambogic acid (10-5-2.5-1.25-0.625-0.3125 µM), trastuzumab (100-50-25-12.5-6.25-3.125 µg/ml) and gambogic acid+trastuzumab were incubated with cells for 12-72 hours at 37 °C in a humidified incubator within an atmosphere containing 5% CO 2 .…”

Section: Cell Proliferation Assaymentioning

confidence: 99%

Investigation of The Synergistic Effects of Trastuzumab And Gambogic Acid in Her-2 Positive Breast Cancer Cell Line

Çetin

Özgür

Kuzucu

et al. 2020

Hacettepe Journal of Biology and Chemistry

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H ER2 pozitif meme kanseri, her yıl milyonlarca ölüme neden olan dünyanın en büyük sağlık sorunlarından biridir. İlaç kombinasyonu modelleme çalışmaları birçok hastalığın tedavisinde kapsamlı bir şekilde değerlendirilmektedir. Son yarım yüzyıl boyunca yapılan farmakolojik çalışmalar, gambojik asidin meme kanseri de dahil olmak üzere birçok kanser türüne karşı güçlü bir anti-tümör aktiviteye sahip olduğunu göstermiştir. Bu çalışmada HER2 pozitif meme kanseri hücre hattında (MDA-MB-453) gambojik asit ve trastuzumabın sinerjistik antikanser etkisini inceledik. Trastuzumab artı gambojik asit çalışmalarının in vitro sinerjistik ve antiproliferatif etkileri XTT yöntemi ile belirlenmiş ve trastuzumab ve gambojik asit kombinasyonunun kombinasyon indeksi (CI) değerleri CompuSyn yazılımı ile hesaplanmıştır. MDA-MB-453 hücrelerinde, trastuzumab ve gambojik asit kombinasyonlarının moleküler mekanizmalarını belirlemek ve HER2, kaspaz-9 ve Bax'ın protein ve gen ekspresyonu seviyelerindeki farklılıklar RT-PCR (qRT-PCR) ve ELISA teknikleri kullanılarak analiz edildi. RT-qPCR ve ELISA testine göre; 50 µg / ml trastuzumab ve 5 µM gambojik asit kombinasyonu, MDA-MB-453 hücre hattında 24 saatlik inkübasyonda en iyi sinerjistik etkiyi gösterdi. Gambojik asitin HER2 pozitif meme kanseri hücre hattı üzerine etkisi, , trastuzumab ile kombinasyonunun meme kanseri hücre proliferasyonunu inhibe eden doğal bileşik potansiyeline sahip olduğunu gösterir.

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“…To measure cell viability, XTT cell proliferation kit was applied according to instructions from the supplier. The IC 50 value of curcumin on Saos-2 cells was calculated with GraphPad Prism 6.0 software [12,13].…”

Section: Cell Proliferation Assaymentioning

confidence: 99%

Kurkumin’in Osteosarkomada Doğal RANKL İnhibitörü Olarak Biyolojik Değerlendirilmesi

Özgür

2020

Türk Doğa Ve Fen Dergisi

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Osteosarcoma is an important health problem among children and teenagers. Metastases is observed in about twenty percent of osteosarcoma patients. RANK/RANKL/OPG signaling pathway is involved in formation of osteosarcoma and its metastases. Especially, the overexpression of RANKL is related to osteoclast and osteosarcoma formation. Therefore, inhibition of RANKL activity has been significant treatment method of osteosarcoma. In this study, curcumin was evaluated as RANKL inhibitor in osteosarcoma cells. In this context, antiproliferative and anti-invasive properties of the curcumin were determined with in-vitro and computational assays in Saos-2 cell line. Obtained results showed that curcumin may have a potential for treatment of osteosarcoma and its metastases.

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Design, Synthesis, and Evaluation of Heat Shock Protein 90 Inhibitors in Human Breast Cancer and Its Metastasis

Abstract: Benzodiazepine derivatives presented here display anticancer activity. The compounds effect on both breast cancer and endothelial cell lines show their potential as drug templates to inhibit breast cancer and its metastasis.

Cited by 21 publications

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Enamines and Dimethylamino Imines as Building Blocks in Heterocyclic Synthesis: Reactions of DMF‐DMA Reagent with Different Functional Groups

Enamines and Dimethylamino Imines as Building Blocks in Heterocyclic Synthesis: Reactions of DMF‐DMA Reagent with Different Functional Groups

Investigation of The Synergistic Effects of Trastuzumab And Gambogic Acid in Her-2 Positive Breast Cancer Cell Line

Kurkumin’in Osteosarkomada Doğal RANKL İnhibitörü Olarak Biyolojik Değerlendirilmesi

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