Quinoline Carboxamide‐Type ABCG2 Modulators: Indole and Quinoline Moieties as Anilide Replacements

Bauer, Stefanie; Ochoa‐Puentes, Cristian; Sun, Qiu; Bause, Manuel; Bernhardt, Günther; König, Burkhard; Buschauer, Armin

doi:10.1002/cmdc.201300319

Cited by 17 publications

(19 citation statements)

References 20 publications

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“…19), testosterone (134,20.1%, Fig. 19), progesterone (28.7%), and androstenedione (135,42.4%, Fig. 19) were the most efficient compounds of this series inhibiting tritiated estrone-sulfate (E 1 S) uptake in a concentration-dependent manner.…”

Section: Acridonesmentioning

confidence: 98%

“…Moreover, compound 149 had no effect on the cell proliferation even at a high concentration of 1 μM, whereas a strong cytostatic effect was observed in combination with topotecan (100 nM). 135 Subsequently, the labile amide and ester groups were replaced by a triazole and a ketone moiety in a bioisosteric approach 136,137 resulting in a 24-hr plasma-stable, ABCG2-selective quinoline-carboxamide type series of very potent modulators. Compound 150 (Fig.…”

Section: G Tariquidar-like Compoundsmentioning

confidence: 99%

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ABCG2/BCRP: Specific and Nonspecific Modulators

Peña-Solórzano

Stark

König

et al. 2016

Medicinal Research Reviews

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Multidrug resistance (MDR) in cancer cells is the development of resistance to a variety of structurally and functionally nonrelated anticancer drugs. This phenomenon has become a major obstacle to cancer chemotherapy seriously affecting the clinical outcome. MDR is associated with increased drug efflux from cells mediated by an energy-dependent mechanism involving the ATP-binding cassette (ABC) transporters, mainly P-glycoprotein (ABCB1), the MDR-associated protein-1 (ABCC1), and the breast cancer resistance protein (ABCG2). The first two transporters have been widely studied already and reviews summarized the results. The ABCG2 protein has been a subject of intense study since its discovery as its overexpression has been detected in resistant cell lines in numerous types of human cancers. To date, a long list of modulators of ABCG2 exists and continues to increase. However, little is known about the clinical consequences of ABCG2 modulation. This makes the design of novel, potent, and nontoxic inhibitors of this efflux protein a major challenge to reverse MDR and thereby increase the success of chemotherapy. The aim of the present review is to describe and highlight specific and nonspecific modulators of ABCG2 reported to date based on the selectivity of the compounds, as many of them are effective against one or more ABC transport proteins.

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Section: Acridonesmentioning

confidence: 98%

Section: G Tariquidar-like Compoundsmentioning

confidence: 99%

ABCG2/BCRP: Specific and Nonspecific Modulators

Peña-Solórzano

Stark

König

et al. 2016

Medicinal Research Reviews

Self Cite

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show abstract

“…Previously, potent and selective ABCB1 and ABCG2 modulators were developed in our laboratory [29][30][31][32][33]. Surprisingly, we identified compounds with inhibitory activity at ABCC1 among substances which were initially synthesized as putative ABCG2…”

Section: A N U S C R I P Tmentioning

confidence: 99%

“…ABCC1 modulation was determined with the calcein-AM microplate assay by analogy with the procedure established for ABCB1 [33]. Briefly, 3-5 days after passaging, the ABCC1 …”

Section: Modulation Of Abcc1mentioning

confidence: 99%