Nitrogen-containing heterocycles as important scaffold for selective and potent HDAC8 inhibition: a step towards effective, non-toxic and selective HDAC8 inhibitor discovery.

Selective inhibition of histone deacetylase 8 (HDAC8) has emerged as a promising approach for treating various diseases, including cancer. However, finding key structural features for HDAC8 inhibition and developing effective and selective HDAC8 inhibitors (HDAC8s) pose significant challenges. In the past few years, the development of various scaffolds for inhibiting HDAC8 has significantly risen and the quest continues.

Derivatives of D(-)-glutamine-based MMP-2 inhibitors as an effective remedy for the management of chronic myeloid leukemia-Part-III: Synthesis, biological screening and in silico binding interaction analysis.

Tyrosine kinase inhibitors (TKIs) have markedly improved the overall survival rate of patients with chronic myeloid leukemia (CML), enabling them to achieve a normal life expectancy. However, toxicity, relapse, and drug resistance continue to pose major challenges in the clinical treatment of CML. The progression of leukemia is directly connected to higher expression levels and enzymatic actions of matrix metalloproteinase-2 (MMP-2).

A Pair of Dinuclear Fe(II) Enantiomers: Syntheses and Structures of ΛΔ/ΔΛ-Bis(Dihydridoborate) Complexes.

In our effort to establish a direct synthetic approach for bis(dihydridoborate) complexes of first-row transition metals, we have investigated the reactivity of [Cp*Fe(dppe)Cl] (dppe =1,2-bis(diphenylphosphino)ethane) with Na[BHL] (L =2-mercaptopyridine (mp) and 2-mercaptobenzothiazole (mbz)) that led to the formation of iron(II) dihydridoborate complexes, [Cp*Fe{κ-S,H,H-(HBH(L))}] 1 a-b (L=mp (1 a) and L=mbz (1 b)). Further, in an attempt to isolate the bis(dihydridoborate) complex of iron by the insertion of borane into the κ-N,S-chelated iron complex, [(dppe)Fe{κ-N,S-(mp)}] (2), we have isolated and structurally characterized a rare example of dimeric iron bis(dihydridoborate) complex, [Fe{κ-S,H,H-(HBH(mp))}], ΛΔ/ΔΛ-3 as pair of enantiomers. Interestingly, these enantiomers ΛΔ/ΔΛ-3 have two trans-[Fe{κ-S,H,H-(HBH(mp))}] moieties bridged through sulfur atoms of 2-mercaptopyridinyl ligands, where the iron centres are hepta-coordinated.

Histone deacetylase 8 in focus: Decoding structural prerequisites for innovative epigenetic intervention beyond hydroxamates.

Histone deacetylase 8 (HDAC8) inhibitors play a pivotal role in epigenetic regulation. Numerous HDAC8 inhibitors (HDAC8is), that are non-hydroxamates have been identified to date, and a few of them exhibit antiproliferative activity that is on par with hydroxamates. While many non-hydroxamate-based HDAC8is have demonstrated selectivity, hydroxamate-based HDAC8is, like Vorinostat and TSA, have a tendency of non-specificity among the different HDAC isoforms.

Metabolite Profiling and Integrated Network Pharmacology Based Mechanism of Benincasa hispida (Thunb.) Cogn. Fruit Against Non-insulin-Dependent Diabetes Mellitus.

Introduction: Benincasa hispida (Thunb.) Cogn. (Cucurbitaceae) is an essential food plant in India possessing antihyperglycemic and antihyperlipidemic activities.