117571-34-3Relevant academic research and scientific papers
N-(PYRIDIN-2-YLSULFONYL)CYCLOPROPANECARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF A CFTR MEDIATED DISEASE
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Page/Page column 235, (2020/07/14)
The invention relates to heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.
Compounds having antitumor and antibacterial properties
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, (2008/06/13)
The novel class of xanthenone-4-acetic acids represented by the general formula (I) STR1 where R1 represents up to two of the groups lower alkyl, halogen, CF3, CN, NO2, NH2, CH2 COOH, OR2,
Potential Antitumor Agents. 61. Structure-Activity Relationships for in Vivo Colon 38 Activity among Disubstituted 9-Oxo-9H-xanthene-4-acetic Acids
Rewcastle, Gordon W.,Atwell, Graham J.,Zhuang, Li,Baguley, Bruce C.,Denny, William A.
, p. 217 - 222 (2007/10/02)
Analogues of 9-oxo-9H-xanthene-4-acetic acid (XAA) bearing small, lipophilic 5-substituents are among the most dose-potent compounds yet reported with the capability of causing hemorrhagic necrosis of implanted colon 38 tumors in mice.To further extend structure-activity relationships among this class of compound, a series of XAA derivatives bearing two small lipophilic groups at various positions have been prepared and evaluated.The 5,6-disubstituted compounds in particular show consistently high levels of both dose potency and activity, suggesting this is the optimal configuration among substituted 9-oxo-9H-xanthene-4-acetic acids.The 5,6-dimethyl and 5-methyl-6-methoxy are the most effective analogues, showing in vivo colon 38 activity comparable to that of FAA at 10-15-fold lower doses and superior activity to FAA at the respective optimal doses, and the former has been selected for detailed evaluation.
Potential Antitumor Agents. 58. Synthesis and Structure-Activity Relationships of Substituted Xanthenone-4-acetic Acids Active against the Colon 38 Tumor in Vivo
Rewcastle, Gordon W.,Atwell, Graham J.,Baguley, Bruce C.,Calveley, Stephen B.,Denny, William A.
, p. 793 - 799 (2007/10/02)
In a search for compounds related to flavoneacetic acid with activity against solid tumors, a series of methyl- methoxy-, chloro, nitro-, and hydroxy-substituted xanthenone-4-acetic acids have been synthesized and evaluated against subcutaneously implanted colon adenocarcinoma 38 in vivo, using a short-term histology assay as a primary screening system.A major goal of this work was to identify compounds with similar profiles of activity to that of flavoneacetic acid but of higher potency.The level of activity of the compounds appeared to depend more on the nature of the substituent than its positioning, in the order Cl > Me, OMe > NO2, OH.However, the potency of the compounds was related much more to the position rather than the nature of the substitution, with 5-substituted compounds being clearly the most dose potent. 5-Methylxanthenone-4-acetic acid has a similar level of activity to that of flavoneacetic acid in the test systems employed but is more than 7-fold as does potent.
