Camptothecin structure simplification elaborated new imidazo[2,1-b]quinazoline derivative as a human topoisomerase I inhibitor with efficacy against bone cancer cells and colon adenocarcinoma.

Camptothecin is a pentacyclic natural alkaloid that inhibits the hTop1 enzyme involved in DNA transcription and cancer cell growth. Camptothecin structure pitfalls prompted us to design new congeners using a structure simplification strategy to reduce the ring extension number from pentacyclic to tetracyclic while maintaining potential stacking of the new compounds with the DNA base pairs at the Top1-mediated cleavage complex and aqueous solubility, as well as minimizing compound-liver toxicity. The principal axis of this study was the verification of hTop1 inhibiting activity as a possible mechanism of action and the elaboration of new simplified inhibitors with improved pharmacodynamic and pharmacokinetic profiling using three structure panels (A-C) of (isoquinolinoimidazoquinazoline), (imidazoquinazoline), and (imidazoisoquinoline), respectively.

Comparison of the ocular ultrasonic and optical biometry devices in the different quality measurements.

Purpose: To compare the reliability and agreement of axial length (AL), anterior chamber depth (ACD), and lens thickness (LT) measurements obtained with optical biometry based on swept-source optical coherence tomography (IOLMaster 700; Carl Zeiss, Germany) and an ultrasound biometry device (Nidek; US-4000 Echoscan, Japan) in different qualities of AL measurement.

Methods: A total of 239 consecutive eyes of 239 cataract surgery candidates with a mean age of 56 ± 14 years were included. The quality measurements were grouped according to the quartiles of SD of the measured AL by IOLMaster 700.

Design, Synthesis, Computational Investigations, and Antitumor Evaluation of -Rhodanine Glycosides Derivatives as Potent DNA Intercalation and Topo II Inhibition against Cancer Cells.

Nitrogen and sulfur glycosylation was carried out via the reaction of rhodanine () with α-acetobromoglucose under basic conditions. Deacetylation of the protected nitrogen nucleoside was performed with CHONa in CHOH without cleavage of the rhodanine ring to afford the deprotected nitrogen nucleoside . Further, deacetylation of the protected sulfur nucleoside was performed with CHONa in CHOH with the cleavage of the rhodanine ring to give the hydrolysis product .

Design, synthesis, molecular modelling and antitumor evaluation of -glucosylated rhodanines through topo II inhibition and DNA intercalation.

In the present study, 5-arylidene rhodanine derivatives , -glucosylation rhodanine , -glucosylation rhodanine , -glucoside rhodanine and -glucosylation 5-arylidene rhodanines were synthesised and screened for cytotoxicity against a panel of cancer cells with investigating the effective molecular target and mechanistic cell death. The anomers were separated by flash column chromatography and their configurations were assigned by NMR spectroscopy. The stable structures of the compounds under study were modelled on a molecular level, and DFT calculations were carried out at the B3LYP/6-31 + G (d,p) level to examine their electronic and geometric features.