66735-22-6Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of AV6 derivatives as novel dual reactivators of latent HIV-1
Ao, Mingtao,Pan, Zhenrui,Qian, Yuqing,Tang, Bowen,Feng, Zeming,Fang, Hua,Wu, Zhen,Chen, Jingwei,Xue, Yuhua,Fang, Meijuan
, p. 17279 - 17292 (2018/05/29)
The "shock and kill" strategy might be a promising therapeutic approach for HIV/AIDS due to the existence of latent viral reservoirs. A major challenge of the "shock and kill" strategy arises from the general lack of clinically effective latency-reversing
Design, synthesis and in vitro antitumor activity of 4-aminoquinoline and 4-aminoquinazoline derivatives targeting EGFR tyrosine kinase
Abouzid, Khaled,Shouman, Samia
, p. 7543 - 7551 (2008/12/23)
Two series of new 6-alkoxy-4-substituted-aminoquinazolines (2-4f) and their bioisoteric quinoline congeners (5-7c) were designed and synthesized. Virtual screening was carried out through docking the designed compounds into the ATP binding site of epidermal growth factor receptor (EGFR) to predict if these compounds have analogous binding mode to the EGFR inhibitors. The newly synthesized compounds were tested in vitro on human breast carcinoma cell line (MCF-7) in which EGFR is highly expressed. Most of the tested compounds exploited potent antitumor activity with IC50 values in the nanomolar range in particular compound 3b which displayed the highest activity among the tested compounds with IC50 equal to 0.13 nmol.
