Due to the biological importance of thienopyrimidine derivatives, we present here a synthetic way for the design of new thienopyrimidines (2‒11) using the precursor 2-(4-Oxo-9-phenyl-7-(p-tolylamino)-3,4-dihydropyrimido[4′,5′:4,5]thieno[2,3-d] pyrimidine-2-yl)acetohydrazide 1. Spectral analyses techniques (IR,¹H NMR, and ¹³C NMR) were utilized to confirm the structures of all synthesized compounds. All the new compounds were screened for their anti-bacterial and anti-inflammatory activity showing significant results compared to the standard drug. A molecular docking approach was utilized to investigate the proposed molecular mechanism of the antibacterial and anti-inflammatory activity of the synthesized compounds. Drug-like properties were analyzed to highlight the potential oral drug candidates.

Histone post-translational modifications (PTMs) regulate numerous cellular processes, including gene transcription, cell division, and DNA damage repair. Most histone PTMs affect the recruitment or exclusion of reader proteins from chromatin. Here, we present a protocol to measure affinity and interaction kinetics between histone peptides and the recombinant protein using Bio-layer interferometry.

Chemotherapeutic drugs are used effectively to manage wide types of malignancies, but their therapeutic use is limited due to their associated hepatic intoxication. The current study sheds light on the effect of phytochemicals berberine (BBR) and umbelliferone (UMB) on methotrexate (MTX)-induced hepatic intoxication. Forty-eight rats were allocated to normal, BBR (50 mg/kg orally for 10 days), UMB (30 mg/kg orally for 10 days), MTX (20 mg/kg at the 5th day), BBR+MTX, and UMB+MTX. With regard to MTX, the results of this investigation reveal potent amelioration of MTX hepatotoxicity by BBR and UMB through reduction of the elevated serum levels of ALT, ALP, AST, and LDH confirmed by the attenuation of histopathological abrasion in liver tissues. BBR and UMB markedly restored antioxidant status. More importantly, BBR resulted in reducing P₃₈ mitogen-activated protein kinase (P₃₈MAPK), nuclear factor kappa-B (NF-κB), and Kelch-like ECH-associated protein 1 (Keap-1) genes and enhanced mRNA expression of Nrf-2 (P < 0.05). Interestingly, in silico studies via molecular docking pinpointed the binding modes of BBR and UMB to the binding pocket residues of P₃₈MAPK, NF-κB, and Keap-1 and demonstrated a promising inhibition of Keap-1, P₃₈MAPK, and NF-κB. BBR and UMB reduced the expression of pro-apoptotic protein Bax and apoptotic protein caspase-3 as well as increased the expression of anti-apoptotic protein Bcl-2. Therefore, BBR and UMB may denote promising therapeutic agents that can avert hepatic intoxication in patients receiving MTX.

The object of the present work is to deduce several important developments in various recursion relations, relevant differential recursion formulas, infinite summation formulas, integral representations, and integral operators for Horn’s hypergeometric functions ?1 and ?2.

In this paper, we establish some fixed point results for αqsp -admissible mappings embedded in L-simulation functions in the context of b-metric-like spaces. As an application, we discuss the existence of a unique solution for fractional hybrid differential equation with multipoint boundary conditions via Caputo fractional derivative of order 1 < α ≤ 2. Some examples and corollaries are also considered to illustrate the obtained results.

In this paper, we establish some fixed point results for αqsp -admissible mappings embedded in L-simulation functions in the context of b-metric-like spaces. As an application, we discuss the existence of a unique solution for fractional hybrid differential equation with multipoint boundary conditions via Caputo fractional derivative of order 1 < α ≤ 2. Some examples and corollaries are also considered to illustrate the obtained results.