106429-59-8Relevant articles and documents
POLYCYCLIC AMINES AS OPIOID RECEPTOR MODULATORS
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Paragraph 0129; 0269, (2018/10/11)
The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.
SUBSTITUTED DIHYDROPYRIDINES AND METHODS OF USE
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Page/Page column 134-135, (2010/11/27)
Compounds are provided that are modulators of the C5a receptor. The compounds are substituted dihydropyridines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activtation of C5a receptors.
2'-Substituted 5-phenylterbenzimidazoles as topoisomerase I poisons
Rangarajan, Meera,Kim, Jung Sun,Jin, Song,Sim, Sai-Peng,Liu, Angela,Pilch, Daniel S.,Liu, Leroy F.,Lavoie, Edmond J.
, p. 1371 - 1382 (2007/10/03)
5-Phenylterbenzimidazole (1) is active as a topoisomerase I poison (topo I) and is cytotoxic to human tumor cells. No cross-resistance was observed for 1 when it was evaluated against the camptothecin-resistant cell line, CPT-K5. Derivatives of 1 substituted at the 2'-position, however, did exhibit cross-resistance to this cell line. The basis for the resistance of this cell line towards CPT is that it possesses a mutant form of topo I. These results suggest that substituents at the 2'-position may be in proximity to the wild-type enzyme. Therefore, we hypothesized that terbenzimidazoles with 2'-substituents could be capable of interacting with the enzyme and thereby influence activity within this class of topo I poisons. 5-Phenylterbenzimidazoles with a hydroxy, hydroxymethyl, mercapto, amino, N-benzoylaminomethyl, chloro, and trifluoromethyl group at the 2'-position were synthesized. In addition, several 2'-ethyl-5-phenylterbenzimidazoles were prepared containing either a methoxy, hydroxy, amino, or N-acetylamino group at the 2-position of the ethyl side-chain. These 2'-substituted 5-phenylterbenzimidazoles were evaluated as topo I poisons and for cytotoxic activity. The presence of a strong electron-withdrawing group at the 2'-position, such as a chloro or trifluoromethyl group, did enhance both topo I poisoning activity and cytotoxicity. Studies on the relative DNA binding affinity of 1 to its 2'-amino and 2'-trifluoromethyl derivatives did exhibit a correlation with their relative differences in biological activity. Copyright (C) 2000 Elsevier Science Ltd.