129833-29-0Relevant academic research and scientific papers
PARP INHIBITORS FOR TREATING CANCER AND ASTHMA
-
, (2020/03/23)
Provided are substituted 8-methylquinazolin-4(3H)-one compounds useful as PARP inhibitors for the treatment of cancer and asthma, as well as pharmaceutical compositions comprising them and methods for their synthesis.
SUBSTITUTED BENZAZINONES AS ANTIBACTERIAL COMPOUNDS
-
, (2017/07/14)
The present invention relates to LpxC antibacterial compounds of Formula (1A), corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions:, compound preparation, treatment methods and uses for bacterial infections, especially those caused by gram-negative bacteria.
INDOLINONE ANALOGUES
-
, (2014/10/16)
The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4, A1 and A2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
INDOLINONE ANALOGUES AS BRD4 INHIBITORS
-
, (2014/10/15)
The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4, A1 and A2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
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.
