Synthesis and Investigation of Therapeutic Potential of Isoform-Specific HDAC8 Inhibitors for the Treatment of Cutaneous T Cell Lymphoma was written by Umamaheswari, Appavoo;Puratchikody, Ayarivan;Hari, Natarajan. And the article was included in Anti-Cancer Agents in Medicinal Chemistry in 2019.Recommanded Product: 106-79-6 This article mentions the following:
The aim of this paper was to synthesis and evaluates HDAC8 isoform specific inhibitors. Based on the preliminary report on the design and in-silico studies of 52 hydroxamic acid derivatives bearing multi-substituent heteroaromatic rings with chiral amine linker, five compounds were shortlisted and synthesized by microwave assisted approach and high yielding synthetic protocol. A series of in-vitro assays in addition to HDAC8 inhibitory activity was used to evaluate the synthesized compounds Serine derivatives I [R = H, MeO, OH; R1 = H, Br; R2 = Me, NH2, MeO] and II exerted the anti-proliferative activities against CTCL cell lines at 20- 100 μM concentrations Both the compounds I and II exhibited μM inhibitory activity against HDAC8. The compound I [R = OH, R1 = Br, R2 = Me] displayed remarkable HDAC8 selectivity superior to that of the standard drug, SAHA with an IC50 at 0.1μM. Simple modifications at different portions of pharmacophore in the hydroxamic acid analogs were effective for improving both HDAC8 inhibitory activity and isoform selectivity. Potent and highly isoform-selective HDAC8 inhibitors were identified. These findings were expedient for further development of HDAC8-selective inhibitors. In the experiment, the researchers used many compounds, for example, Dimethyl decanedioate (cas: 106-79-6Recommanded Product: 106-79-6).
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