Despite phenomenal clinical success, the efficacy of platinum anticancer drugs is often compromised due to inherent and acquired drug resistant phenotypes in cancers. To circumvent this issue, we designed two heterobimetallic platinum (II)-ferrocene hybrids that display multi-pronged anticancer action. In cancer cells, our best compound, 2 , platinates DNA, produces reactive oxygen species, and has nucleus, mitochondria, and endoplasmic reticulum as potential targets. The multi-modal mechanism of action of these hybrid agents lead to non-apoptotic cell death induction which enables circumventing apoptosis resistance and significant improvement in platinum cross resistance profile. Finally, in addition to describing detail mechanistic insights, we also assessed its stability in plasma and demonstrate anticancer efficacy in an in vivo A2780 xenograft model. Strikingly, compared to oxaliplatin, our compound displays better tolerability, safety profile and efficacy in vivo. 相似文献
Russian Journal of Physical Chemistry A - The viscosities of aqueous solutions of L-alanine and L-valine with non-steroid anti-inflammatory drug dolonex (0.020, 0.040, 0.060 mol kg–1) have... 相似文献
A newly designed internal charge transfer chemosensor, DIPZON exhibits Co2+ selective optical responses, which include 112 nm red shift in absorption and a dramatic 37-fold enhancement in the fluorescence output in the buffer CH3OH/H2O (1:1 v/v) system. By contrast, the optical responses were not as sensitive with several other biologically relevant metal ions examined with the binding interactions following the sequence Co2+ > Cu2+ > Zn2+ > Cd2+ >> Ba2+ ≈ Ca2+ ≈ Mg2+ ≈ K+ ≈ Na+ ≈ Li+. 相似文献
We have developed an efficient non-ionic surfactant (Triton X-100) catalyzed multicomponent synthesis of Betti base from secondary amine, aromatic aldehydes, and β-naphthol using Mannich-type reaction in water. Lewis and Brønsted acid catalysts, ionic and non-ionic surfactant have been screened for the reaction. Non-ionic surfactant (Triton X-100) gave the best results and the reaction proceeds through the imine formation, which is stabilized by colloidal dispersion and undergoes nucleophilic addition to afford the corresponding N,N-dialkylated Betti base in excellent yields. 相似文献
The present work aims to assess health risks associated with the exposure to uranium and heavy metals via potable groundwater in Uttarakhand state of India. For this purpose, potable groundwater samples were collected from the area and analyzed using LED fluorimetry and inductively coupled plasma mass spectrometry (ICPMS). The radiological (carcinogenic) and chemical (non-carcinogenic) risks associated with the exposure to uranium in majority of locations were observed below the safe limits suggested by WHO and USEPA. The levels of heavy metals present in potable groundwater were found well below the permissible limits recommended by WHO. An inter-comparison exercise between the results obtained with LED fluorimetry and ICPMS techniques was performed for the assurance of reliability and accuracy of results. The results were found in good agreement with each other.
Herein, we summarize the synthetic approaches that have been developed for the synthesis of star‐shaped molecules. Typically, to design such highly functionalized molecules, simple building blocks are first assembled through trimerization reactions, starting from commercially available starting materials. Then, these building blocks are synthetically manipulated to generate extended star‐shaped molecules. We also discuss the syntheses of star‐shaped molecules that contain 2,4,6‐trisubstituted 1,3,5‐triazine or 1,3,5‐trisubstituted benzene rings as a central core and diverse substituted styrene, phenyl, and fluorene derivatives at their periphery, which endows these molecules with extended conjugation. A variety of metal‐catalyzed reactions, such as Suzuki, Buchwald–Hartwig, Sonogashira, Heck, and Negishi cross‐coupling reactions, as well as metathesis, have been employed to functionalize a range of star‐shaped molecules. The methods described herein will be helpful for designing a wide range of intricate compounds that are highly valuable in the fields of supramolecular chemistry and materials science. Owing to space limitations, we will not cover all of the publications on this topic. Instead, we will focus on examples that were reported by our research group and other relevant recent literature. Apart from the trimerization sequence, this Minireview has been structured based on the key reactions that were used to prepare the star‐shaped molecules and other higher analogues. Finally, some examples that do not fit into this classification are discussed. 相似文献
An efficient multicomponent synthesis of Ugi compounds comprising coumarin backbone has been achieved by employing one pot five component sequential Knoevenagel-Ugi reaction. This method offers the advantages of easy handling procedure, atom economy, mild reaction conditions and good yields of products. A molecular library was synthesized by changing the substituents on two of the independent starting materials. The synthesized compounds were also tested for anti-microbial activities and were found to be moderate to good anti-bacterial agents. 相似文献
Laser Raman spectroscopy was employed as a non-destructive probe for the detection and monitoring of crystalline arsenic in
the native oxide films formed during heating of GaAs in air at various temperatures. Spectroscopy of oxide films formed after
successive heating and etching treatments could confirm the location of arsenic to be near the top of the GaAs: native oxide
overlayer. 相似文献