9H-carbazole derivatives from a Streptomyces species under potassium iodide stress and their anti-inflammatory properties.

By continuously activating silent gene cluster of the marine-derived Streptomyces strain OUCMDZ-5511 under high salt stress, three new iodinated 9H-carbazole derivatives (1-3) and a novel oxazole-fused chlorinated 9H-carbazole derivative (4), along with five previously reported analogues (5-9), were obtained from the cultures grown with 7.5% potassium iodide (KI). The structures of these previously undocumented compounds were elucidated as 4-iodo-3-methoxy-9H-carbazole (1), 4-iodo-3-methoxy-9H-carbazole-6-ol (2), 4-iodo-3-methoxy-9H-carbazole-8-ol (3), and 10-chloro-9-methoxy-6H-oxazolo[5,4-c]carbazole (4), using MS and NMR spectroscopic techniques.

Design, synthesis and biological evaluation of 2,3-dihydro-[1,4]dioxino[2,3-f]quinazoline derivatives as EGFR inhibitors.

Epidermal growth factor receptor (EGFR) is the most attractive target for drug research in non-small cell lung cancer (NSCLC). The first-generation EGFR tyrosine kinase inhibitors (TKIs) Gefetinib and Elotinib showed good clinical efficacy on lung adenocarcinoma tumors, but almost all patients developed resistance to these inhibitors over time. Quinazoline and quinoline derivatives are common targeted inhibitors of EGFR kinase, and their structural optimization is an important direction for the development of effective targeted anticancer drugs.