34545-25-0Relevant articles and documents
OXADIAZOLE DERIVATIVES AND PHARMACEUTICAL USES THEREOF
-
Paragraph 0227-0228, (2017/02/02)
PROBLEM TO BE SOLVED: To provide therapeutic or preventive agents for various diseases or symptoms associated with a serotonin 4 receptor (particularly, neuropsychiatric diseases such as Alzheimer-type dementia). SOLUTION: The present invention provides a compound represented by formula (1) or a pharmaceutically acceptable salt thereof. In the formula (1), Het represents formula (Het-1) or the like, A represents formula (A-1) or the like, B represents (B-1) or the like, R1A represents a hydrogen atom, an alkyl group or the like, R2A, R5, R6 and R7 represent a hydrogen atom, a halogen atom, an alkyl group or the like, R8 and R9 represent a hydrogen atom, an alkyl group or the like, and l represents an integer of 0-4. SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
Potential Antitumor Agents. 59. Structure-Activity Relationships for 2-Phenylbenzimidazole-4-carboxamides, a New Class of "Minimal" DNA-Intercalating Agents Which May Not Act via Topoisomerase II
Denny, William A.,Rewcastle, Gordon W.,Baguley, Bruce C.
, p. 814 - 819 (2007/10/02)
A series of substituted 2-phenylbenzimidazole-4-carboxamides has been synthesized and evaluated for in vitro and in vivo antitumor activity.These compounds represent the logical conclusion to our search for "minimal" DNA-intercalating agents with the lowest possible DNA-binding constants.Such "2-1" tricyclic chromophores, of lower aromaticity than the structurally similar 2-phenylquinolines, have the lowest DNA binding affinity yet seen in the broad series of tricyclic carboxamide intercalating agents.Despite very low in vitro cytotoxicities, several of the compoundshad moderate levels of in vivo antileukemic effects.However, the most interesting aspect of their biological activity was the lack of cross-resistance shown to an amsacrine-resistant P388 cell line, suggesting that these compounds may not express their cytotoxicity via interaction with topoisomerase II.