857208-58-3Relevant articles and documents
PROCESS FOR THE SYNTHESIS OF IVACAFTOR AND RELATED COMPOUNDS
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Paragraph 062-063, (2016/12/01)
The present patent discloses a novel one pot two-step process for the synthesis of ivacaftor and related compounds of [Formula (I)], wherein R1, R2, R3, R4, R5, R6, R7 and Ar1 are as described above; its tautomers or pharmaceutically acceptable salts thereof starting from indole acetic acid amides.
Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases
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, (2015/09/22)
The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
Synthesis, cytotoxicity and mechanistic evaluation of 4-oxoquinoline-3- carboxamide derivatives: Finding new potential anticancer drugs
Forezi, Luana Da S. M.,Tolentino, Nathalia M. C.,De Souza, Alessandra M. T.,Castro, Helena C.,Montenegro, Raquel C.,Dantas, Rafael F.,Oliveira, Maria E. I. M.,Silva Jr., Floriano P.,Barreto, Leilane H.,Burbano, Rommel M. R.,Abrahim-Vieira, Barbara,De Oliveira, Riethe,Ferreira, Vitor F.,Cunha, Anna C.,Boechat, Fernanda Da C. S.,De Souza, Maria Cecilia B. V.
, p. 6651 - 6670 (2014/06/10)
As part of a continuing search for new potential anticancer candidates, we describe the synthesis, cytotoxicity and mechanistic evaluation of a series of 4-oxoquinoline-3-carboxamide derivatives as novel anticancer agents. The inhibitory activity of compounds 10-18 was determined against three cancer cell lines using the MTT colorimetric assay. The screening revealed that derivatives 16b and 17b exhibited significant cytotoxic activity against the gastric cancer cell line but was not active against a normal cell line, in contrast to doxorubicin, a standard chemotherapeutic drug in clinical use. Interestingly, no hemolytical activity was observed when the toxicity of 16b and 17b was tested against blood cells. The in silico and in vitro mechanistic evaluation indicated the potential of 16b as a lead for the development of novel anticancer agents against gastric cancer cells.
