Elkamhawy, Ahmed published the artcileTargeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking, Name: 3-Chloro-4-fluoronitrobenzene, the publication is Bioorganic & Medicinal Chemistry Letters (2015), 25(22), 5147-5154, database is CAplus and MEDLINE.
Coexpression of EGFR and HER2 has been found in many tumors such as breast, ovarian, colon and prostate cancers, with poor prognosis of the patients. Herein, our team has designed and synthesized new eighteen compounds with 6-substituted 4-anilinoquinazoline core to selectively inhibit EGFR/HER2 tyrosine kinases. Twelve compounds showed nanomolar range of IC50 values on EGFR and/or HER2 kinases. Accordingly, a detailed structure activity relationship (SAR) was established. A mol. docking study demonstrated the favorable binding modes of I (X = Me, NHEt) at the ATP active site of both kinases. A kinase selectivity profile performed for compound 8d showed great selectivity for EGFR and HER2. In addition, compound I (X = Me, NHEt) and II exerted selective promising cytotoxic activity over BT-474 cell line with IC50 values of 2.70, 1.82 and 1.95 μM, resp. From these results, we report analogs I (X = Me, NHEt) and II as promising candidates for the discovery of well-balanced compounds in terms of the kinase inhibitory potency and antiproliferative activity.
Bioorganic & Medicinal Chemistry Letters published new progress about 350-30-1. 350-30-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Nitro Compound,Benzene, name is 3-Chloro-4-fluoronitrobenzene, and the molecular formula is C6H3ClFNO2, Name: 3-Chloro-4-fluoronitrobenzene.
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