Category: isothiazole. I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Targeting EGFR tyrosine kinase: Synthesis, in vitro antitumor evaluation, and molecular modeling studies of benzothiazole-based derivatives published in 2020.0, Reprint Addresses Ghaly, MA (corresponding author), Mansoura Univ, Dept Med Chem, Fac Pharm, Mansoura 35516, Egypt.. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde.
New benzothiazole-based derivatives were synthesized in the present work with the aim of evaluating their antitumor activity. They were in vitro tested against hepatocellular carcinoma (HepG2), colorectal carcinoma (HCT-116), mammary gland cancer (MCF-7), prostate cancer (PC-3), and epithelioid carcinoma (HeLa). The results of the in vitro antitumor evaluation revealed that the most active compounds were 39, 40, 51, 56, and 61 exhibiting IC50 values comparable to the reference drug lapatinib. The most active compounds were further subjected to EGFR inhibitory activity assay to rationalize their potency mode. Notably, the most active antitumor compounds 39 and 40 represented the most potent inhibitors to EGFR with IC50 values of 24.58 and 30.42 nM respectively in comparison with 17.38 nM for lapatinib as a standard drug. Molecular modeling studies were also conducted for the synthesized compounds, including docking into EGFR active site and surface mapping. Results proved the superior binding of the hydrazone derivatives 39 and 40 with EGFR suggesting them as good candidates for targeted antitumor therapy through EGFR kinase inhibition.
Category: isothiazole. Welcome to talk about 93-02-7, If you have any questions, you can contact Mokhtar, AM; El-Messery, SM; Ghaly, MA; Hassan, GS or send Email.
Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com