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Relevant academic research and scientific papers

Fabrication of furan-functionalized quinazoline hybrids: Their antibacterial evaluation, quantitative proteomics, and induced phytopathogen morphological variation studies

The limited number of agrochemicals targeting plant bacterial diseases has driven us to develop highly efficient, low-cost, and versatile antibacterial alternatives. Herein, a novel type of simple furan-functionalized quinazolin-4-amines was systematically fabricated and screened for their antibacterial activity. Bioassay results revealed that compounds C1 and E4 could substantially block the growth of two frequently mentioned pathogens Xanthomonas oryzae pv oryzae and X. axonopodis pv citri in vitro, displaying appreciable EC50 values of 7.13 and 10.3 mg/L, respectively. This effect was prominently improved by comparing those of mainly used agrochemicals. An in vivo experiment against bacterial blight further illustrated their viable applications as antimicrobial ingredients. Quantitative proteomics demonstrated that C1 possessed a remarkable ability to manipulate the upregulation and downregulation of expressed proteins, which probably involved d-glucose and biotin metabolic pathways. This finding was substantially verified by parallel reaction monitoring analysis. Scanning electron microscopy images and fluorescence spectra also indicated that the designed compounds had versatile capacities for destroying the integrity of bacteria. Given these remarkable characteristics, furan-functionalized quinazoline hybrids can serve as a viable platform for developing innovative antibiotic alternatives against bacterial infections.

COMBINATION WITH CHECKPOINT INHIBITORS TO TREAT CANCER

A combination comprising a compound of Formula (I) and/or Formula (Ia), or a pharmaceutically acceptable salt thereof, and at least one immune checkpoint modulator. Methods for the prevention and treatment of a cancer comprises administering to a subject in need thereof, a therapeutically effective amount of a combination, the combination comprising: a compound of Formula (I) and/or Formula (Ia), or a pharmaceutically acceptable salt thereof, and at least one immune checkpoint modulator.

4-Amino quinazoline compound as well as preparation method and application thereof

The invention relates to a 4-amino quinazoline compound as well as a preparation method and application thereof. The compound has a general formula I) as shown in the specification, a quinazoline compound is taken as a basis, an aromatic ring methylene is introduced into the system for synthesizing a series of aromatic ring-containing methylene substituted 4-amino quinazoline compounds, the compound has a good inhibiting effect on pathogenic bacteria of plants, and has a good inhibiting effect on pathogenic bacteria such as xanthomonas oryzae, Xanthomonas citri and the like.

SMALL MOLECULE INHIBITORS OF EGFR AND PI3K

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quinazoline structure or a quinoline structure which function as dual inhibitors of EGFR proteins and PI3K proteins, and their use as therapeutics for the treatment of cancer and other diseases.