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1,2,3,4-Tetrahydroisoquinoline/2H-chromen-2-one conjugates as nanomolar P-glycoprotein inhibitors: Molecular determinants for affinity and selectivity over multidrug resistance associated protein 1.
Rullo M, Niso M, Pisani L, Carrieri A, Colabufo NA, Cellamare S, Altomare CD. Rullo M, et al. Eur J Med Chem. 2019 Jan 1;161:433-444. doi: 10.1016/j.ejmech.2018.10.043. Epub 2018 Oct 18. Eur J Med Chem. 2019. PMID: 30384046
Linker length and flexibility played a key role in enhancing P-gp affinity as proved by the most potent P-gp modulator (3h, IC(50) = 70 nM). A phenyl ring within the spacer (3k, 3l, 3o) and bulkier groups (Br in 3r, Ph in 3u) at coumarin C3 led to deri …
Linker length and flexibility played a key role in enhancing P-gp affinity as proved by the most potent P-gp modulator (3h, IC …
Transplantation of spinal cord-derived neural stem cells for ALS: Analysis of phase 1 and 2 trials.
Glass JD, Hertzberg VS, Boulis NM, Riley J, Federici T, Polak M, Bordeau J, Fournier C, Johe K, Hazel T, Cudkowicz M, Atassi N, Borges LF, Rutkove SB, Duell J, Patil PG, Goutman SA, Feldman EL. Glass JD, et al. Neurology. 2016 Jul 26;87(4):392-400. doi: 10.1212/WNL.0000000000002889. Epub 2016 Jun 29. Neurology. 2016. PMID: 27358335 Free PMC article. Clinical Trial.
All participants received bilateral injections into the cervical spinal cord (C3-C5). The final group received injections into both the lumbar (L2-L4) and cervical cord through 2 separate surgical procedures. ...
All participants received bilateral injections into the cervical spinal cord (C3-C5). The final group received injections into both t …
Antitumour activity of novel taxanes that act at the same time as cytotoxic agents and P-glycoprotein inhibitors.
Ferlini C, Distefano M, Pignatelli F, Lin S, Riva A, Bombardelli E, Mancuso S, Ojima I, Scambia G. Ferlini C, et al. Br J Cancer. 2000 Dec;83(12):1762-8. doi: 10.1054/bjoc.2000.1500. Br J Cancer. 2000. PMID: 11104578 Free PMC article.
We investigated, on a panel of 7 human cancer cell lines, the growth inhibition effect of 3 newly developed taxanes (SB-T-1213, SB-T-1250 and SB-T-101187) with modification at the C10 and C3' positions of the taxane framework. These positions have been previously character …
We investigated, on a panel of 7 human cancer cell lines, the growth inhibition effect of 3 newly developed taxanes (SB-T-1213, SB-T-1250 an …