1248541-99-2Relevant academic research and scientific papers
Contrasting sirtuin and poly(ADP-ribose)polymerase activities of selected 2,4,6-trisubstituted benzimidazoles
Yeong, Keng Yoon,Tan, Soo Choon,Mai, Chun-Wai,Leong, Chee-Onn,Chung, Felicia Fei-Lei,Lee, Yean Kee,Chee, Chin Fei,Abdul Rahman, Noorsaadah
, p. 213 - 219 (2018)
Both sirtuin and poly(ADP-ribose)polymerase (PARP) family of enzymes utilize NAD+ as co-substrate. Inhibitors of sirtuins and PARPs are important tools in drug discovery as they are reported to be linked to multiple diseases such as cancer. New potent sirtuin inhibitors (2,4,6-trisubstituted benzimidazole) were discovered from reported PARP inhibitor scaffold. Interestingly, the synthesized compounds have contrasting sirtuin and PARP-1 inhibitory activities. We showed that modification on benzimidazoles may alter their selectivity toward sirtuin or PARP-1 enzymes. This offers an opportunity for further discovery and development of new promising sirtuin inhibitors. Molecular docking studies were carried out to aid the rationalization of these observations. Preliminary antiproliferative studies of selected compounds against nasopharyngeal cancer cells also showed relatively promising results.
Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH
Abdullah, Iskandar,Chee, Chin Fei,Lee, Yean-Kee,Thunuguntla, Siva Sanjeeva Rao,Satish Reddy,Nellore, Kavitha,Antony, Thomas,Verma, Jitender,Mun, Kong Wai,Othman, Shatrah,Subramanya, Hosahalli,Rahman, Noorsaadah Abd.
, p. 4669 - 4680 (2015/08/03)
Poly (ADP-ribose) polymerases (PARPs) play diverse roles in various cellular processes that involve DNA repair and programmed cell death. Amongst these polymerases is PARP-1 which is the key DNA damage-sensing enzyme that acts as an initiator for the DNA
DIHYDROOROTATE DEHYDROGENASE INHIBITORS
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Page/Page column 98, (2010/11/03)
The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
