2015
DOI: 10.1016/j.bmc.2015.05.051
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Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH

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Cited by 44 publications
(15 citation statements)
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“…In their studies, the biphenyl ring system was retained for activity and the substitution pattern (-F, -CF 3 and -OCF 3 ) on the biphenyl ring system was the most significant feature for better human DHODH inhibitory activity. Similar results were drawn by Abdullah (Abdullah et al, 2015) and Batt (Batt et al, 1998). It should be mentioned that in some investigations, the biphenyl ring system or biphenyl with an additional linker system reduced inhibitory activity because of the steric constraints of the binding pocket in this area (Zhu et al, 2015).…”
Section: Design and Dockingsupporting
confidence: 79%
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“…In their studies, the biphenyl ring system was retained for activity and the substitution pattern (-F, -CF 3 and -OCF 3 ) on the biphenyl ring system was the most significant feature for better human DHODH inhibitory activity. Similar results were drawn by Abdullah (Abdullah et al, 2015) and Batt (Batt et al, 1998). It should be mentioned that in some investigations, the biphenyl ring system or biphenyl with an additional linker system reduced inhibitory activity because of the steric constraints of the binding pocket in this area (Zhu et al, 2015).…”
Section: Design and Dockingsupporting
confidence: 79%
“…Through modulating pyrimidine biosynthesis, inhibitors of dihydroorotate dehydrogenase (DHODH) have proved to be clinically useful in the treatment of autoimmune diseases such as rheumatoid arthritis, multiple sclerosis, transplant rejection and psoriatic arthritis (Norman, 2013;Munier-Lehmann et al, 2013). Many inhibitors have also been investigated to treat cancer (Dell, 1998;Hurt et al, 2006;Vyas et al, 2014;Abdullah et al, 2015) and viral (Zhang et al, 2012) and parasite infections (i.e. malaria) (Seymour et al, 1994;Booker et al, 2010;Skerlj et al, 2011), as well being used as antifungal agents (Gustafson et al, 1996), antibiotics (Marcinkeviciene et al, 2000;Copeland et al, 2000) and in crop science (Longhurst et al, 1996).…”
Section: Introductionmentioning
confidence: 99%
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“…Also it exhibited inhibition of tubulin polymerisation upto 71.27% with IC 50 values 1.71 μM against nocodazole (1.75 µM) as the standard drug. Abdullah et al carried out the synthesis of new benzimidazole derivatives as potential dual inhibitors for PARP‐1 and dihydroorotate dehydrogenase (DHODH) enzymes (Schemes and ). Compounds 318c and 316b showed most potent results against veliparib and brequinar as reference inhibitors.…”
Section: Pharmacological and Synthetic Profiles Of Benzimidazole Derimentioning
confidence: 99%
“…Together, the observation of prolonged S-phase arrest, the upregulation of the DDR response in HHQ-exposed cultures, the conserved nature of the mammalian and E. huxleyi PARP catalytic site (Fig. S16), and the chemical structural similarities of HHQ to known inhibitors of both PARP and DHODH with core benzimidazole moieties 51 , collectively suggest that HHQ may function simultaneously to inhibit both PARP and DHODH activity in E. huxleyi.…”
Section: Hhqmentioning
confidence: 93%