Recently I am researching about SELECTIVE HDAC3 INHIBITORS; CANCER; FAMILY, Saw an article supported by the Science and Engineering Research Board, Department of Science and Technology (SERB-DST), New Delhi, IndiaDepartment of Science & Technology (India) [EMR/2016/001411]. Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Hamoud, MMS; Pulya, S; Osman, NA; Bobde, Y; Hassan, AEA; Abdel-Fattah, HA; Ghosh, B; Ghanim, AM. The CAS is 100-83-4. Through research, I have a further understanding and discovery of 3-Hydroxybenzaldehyde. Quality Control of 3-Hydroxybenzaldehyde
Most of the FDA approved histone deacetylase inhibitors (HDACi) contain hydroxamate as the zinc binding group (ZBG). Hydroxamates form strong electrostatic metal chelation with divalent zinc present in HDAC. This strong zinc chelation leads to unwanted metabolic abnormalities. Therefore, the design of a non-hydroxamate moiety as a ZBG encourages medicinal chemistry researchers. Here, a series of nicotinamide derivatives have been designed and synthesized as HDACi. All compounds were tested for their inhibitory activities against pan HDACs (containing predominantly HDAC1 and HDAC2 isozymes) and against the HDAC3 isoform. Among these, compounds6band6nshowed comparable pan HDAC inhibitory activity (IC50= 4.648 mu M and IC50= 5.481 mu M, respectively) compared withBG45(IC50= 5.506 mu M). Compound6bexhibited the best potency against HDAC3 with IC50= 0.694 mu M. In addition, the anti-proliferative activity of the synthesized compounds6a-swas evaluated against three different cancer cell lines including B16F10, MCF-7, and A549. Compound6bdisplayed the highest anti-proliferative potency (IC50= 4.66 mu M in B16F10 cell lines) and compounds6b,6c,6h,6i,6l,6m, and6nexhibited higher cytotoxicity against all cell lines compared with the referenceBG45. The selected potent compounds also displayed significant selectivity against cancer cell lines over normal human embryonic kidney (HEK-293) cell lines. The molecular modelling study displayed possible interactions between the most potent inhibitor6band HDAC3 active sites. Furthermore, the predictedin silicostudies of all target compounds revealed acceptable physicochemical properties and pharmacokinetic parameters.
Quality Control of 3-Hydroxybenzaldehyde. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Hamoud, MMS; Pulya, S; Osman, NA; Bobde, Y; Hassan, AEA; Abdel-Fattah, HA; Ghosh, B; Ghanim, AM or concate me.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles