Design, synthesis and antitumor activity of 4-indazolylpyrimidine derivatives as EGFR inhibitors.

To overcome T790M mutation, a novel series of 4-indazolypyrimidine derivatives were developed as novel EGFR inhibitors employing a scaffold hopping drug design strategy. The biological activities of the target compounds were evaluated against two tumor cell lines (A431 and NCI-H1975), normal cell 2BS and EGFR kinase. The results indicated that the majority of the compounds exhibited promising antitumor activity and low toxicity.

Synthesis of Quinolinoneylnitrones and Coumarinylnitrones via a Cascade Hydroamination and Aza-MBH-Type Reaction.

Nitrones are quite useful intermediates and have been broadly applied in organic synthesis, drug discovery, and photochemistry research. Many functional nitrones have been successfully prepared using various strategies. In this work, an efficient method for synthesizing novel quinolinoneylnitrone and coumarinylnitrone derivatives was developed.

Design, synthesis and antitumor activity of 4-arylamine substituted pyrimidine derivatives as noncovalent EGFR inhibitors overcoming C797S mutation.

Clinical researches have shown that epidermal growth factor receptor (EGFR) is a key target for treatment of non-small cell lung cancer (NSCLC). Many EGFR inhibitors were successfully developed as ani-tumor drugs to treat NSCLC patients. Unfortunately, drug resistances were found in clinic.

Design, synthesis and biological evaluation of 4-arylamino-pyrimidine derivatives as focal adhesion kinase inhibitors.

A novel series of 4-arylamino-pyrimidine derivatives were designed and synthesized as focal adhesion kinase (FAK) inhibitors under the strategy of structure-based drug design. Most compounds performed excellent anti-proliferative activity against U87-MG cells. Especially, compounds 8d and 9b revealed the highest activity with IC values of 0.

Discovery of 4-nitro-3-phenylisoxazole derivatives as potent antibacterial agents derived from the studies of [3 + 2] cycloaddition.

Polysubstituted phenylisoxazoles were designed and synthesized to discover new antibacterial agents [3 + 2] cycloaddition. Thirty-five compounds with a phenylisoxazole scaffold were characterized by NMR, HRMS, and X-ray techniques. After being evaluated against (), (), and (), 4-nitro-3-phenylisoxazole derivatives were found to better antibacterial activities.