Matches in SemOpenAlex for { <https://semopenalex.org/work/W1990996412> ?p ?o ?g. }
- W1990996412 endingPage "9491" @default.
- W1990996412 startingPage "9467" @default.
- W1990996412 abstract "A SAR study has been carried out around a modified scaffold of the natural product psammaplin A obtained by replacing the o-bromophenol unit by an indole ring. A series of indole psammaplin A constructs were generated in a short synthetic sequence that starts with the functionalization of the C3 indole position with in situ generated nitrosoacrylate, and this is followed by protection of the β-indole-α-oximinoesters, saponification, condensation with symmetrical diamines, and deprotection. Biochemical and cellular characterization using U937 and MCF-7 cells confirmed that many of these analogues displayed more potent actitivies than the parent natural product. Moreover, in addition to the reported HDAC and DNMT dual epigenetic inhibitory profile of the parent compound, some analogues, notably 4a (UVI5008), also inhibited the NAD(+)-dependent SIRT deacetylase enzymes. The SAR study provides structural insights into the mechanism of action of these multiple epigenetic ligands and paves the way for additional structural exploration to optimize their pharmacological profiles. Because of their multi(epi)target features and their action in ex vivo samples, the indole-based psammaplin A derivatives are attractive molecules for the modulation of epigenetic disorders." @default.
- W1990996412 created "2016-06-24" @default.
- W1990996412 creator A5009160904 @default.
- W1990996412 creator A5014308020 @default.
- W1990996412 creator A5014727489 @default.
- W1990996412 creator A5023140151 @default.
- W1990996412 creator A5036095832 @default.
- W1990996412 creator A5039682482 @default.
- W1990996412 creator A5044999679 @default.
- W1990996412 creator A5055816753 @default.
- W1990996412 creator A5070580222 @default.
- W1990996412 creator A5078908851 @default.
- W1990996412 creator A5079599826 @default.
- W1990996412 creator A5086152631 @default.
- W1990996412 creator A5070656477 @default.
- W1990996412 date "2012-10-17" @default.
- W1990996412 modified "2023-09-25" @default.
- W1990996412 title "Indole-Derived Psammaplin A Analogues as Epigenetic Modulators with Multiple Inhibitory Activities" @default.
- W1990996412 cites W1965262464 @default.
- W1990996412 cites W1967408138 @default.
- W1990996412 cites W1968826316 @default.
- W1990996412 cites W1969820630 @default.
- W1990996412 cites W1972649718 @default.
- W1990996412 cites W1973118113 @default.
- W1990996412 cites W1973677698 @default.
- W1990996412 cites W1974058617 @default.
- W1990996412 cites W1974436842 @default.
- W1990996412 cites W1976161355 @default.
- W1990996412 cites W1976499671 @default.
- W1990996412 cites W1980937575 @default.
- W1990996412 cites W1981259598 @default.
- W1990996412 cites W1982886249 @default.
- W1990996412 cites W1983525029 @default.
- W1990996412 cites W1984807040 @default.
- W1990996412 cites W1985169246 @default.
- W1990996412 cites W1985444222 @default.
- W1990996412 cites W1985515161 @default.
- W1990996412 cites W1987189614 @default.
- W1990996412 cites W1993397999 @default.
- W1990996412 cites W1995511322 @default.
- W1990996412 cites W1996395636 @default.
- W1990996412 cites W1996487270 @default.
- W1990996412 cites W1998470347 @default.
- W1990996412 cites W1999826026 @default.
- W1990996412 cites W2000809959 @default.
- W1990996412 cites W2004172747 @default.
- W1990996412 cites W2008978345 @default.
- W1990996412 cites W2009649161 @default.
- W1990996412 cites W2009825624 @default.
- W1990996412 cites W2012508649 @default.
- W1990996412 cites W2015735594 @default.
- W1990996412 cites W2016849135 @default.
- W1990996412 cites W2024074798 @default.
- W1990996412 cites W2024751945 @default.
- W1990996412 cites W2024966097 @default.
- W1990996412 cites W2026597757 @default.
- W1990996412 cites W2028733293 @default.
- W1990996412 cites W2029215475 @default.
- W1990996412 cites W2030946593 @default.
- W1990996412 cites W2031598870 @default.
- W1990996412 cites W2032264423 @default.
- W1990996412 cites W2032919244 @default.
- W1990996412 cites W2033102369 @default.
- W1990996412 cites W2034168619 @default.
- W1990996412 cites W2036158314 @default.
- W1990996412 cites W2038109886 @default.
- W1990996412 cites W2042749688 @default.
- W1990996412 cites W2046387526 @default.
- W1990996412 cites W2046934643 @default.
- W1990996412 cites W2047563414 @default.
- W1990996412 cites W2051615431 @default.
- W1990996412 cites W2053213384 @default.
- W1990996412 cites W2055539528 @default.
- W1990996412 cites W2055991021 @default.
- W1990996412 cites W2056605533 @default.
- W1990996412 cites W2059183805 @default.
- W1990996412 cites W2064944074 @default.
- W1990996412 cites W2065583248 @default.
- W1990996412 cites W2068078666 @default.
- W1990996412 cites W2073546855 @default.
- W1990996412 cites W2080653934 @default.
- W1990996412 cites W2081614272 @default.
- W1990996412 cites W2081685122 @default.
- W1990996412 cites W2082971158 @default.
- W1990996412 cites W2084366893 @default.
- W1990996412 cites W2089112805 @default.
- W1990996412 cites W2089626640 @default.
- W1990996412 cites W2091007186 @default.
- W1990996412 cites W2091685314 @default.
- W1990996412 cites W2091799485 @default.
- W1990996412 cites W2092488358 @default.
- W1990996412 cites W2093522968 @default.
- W1990996412 cites W2095199845 @default.
- W1990996412 cites W2096083625 @default.
- W1990996412 cites W2098536205 @default.
- W1990996412 cites W2099803844 @default.
- W1990996412 cites W2100645337 @default.
- W1990996412 cites W2102159603 @default.