Cheng, Jie; Zhao, Wei; Yao, Hui; Shen, Yuemao; Zhang, Youming; Li, Yue-zhong; QI, Qingsheng; Wongprasert, Kanokpan; Tang, Ya-Jie published the artcile< Discovery of 4,6-O-Thenylidene-β-D-glucopyranoside-(2''-acetamido, 3''-acetyl-di-S-5-fluorobenzothizole/5-fluorobenzoxazole)-4'-demethylepipodophyllotoxin as Potential Less Toxic Antitumor Candidate Drugs by Reducing DNA Damage and Less Inhibition of PI3K>, Related Products of 13451-78-0, the main research area is teniposide derivative preparation structure cancer toxicity.
As an FDA-approved drug, teniposide, was utilized in cancer treatment but was accompanied by a strong side effect in long-term clin. trials. This work discovered potential candidate drugs with low toxicity by modifying the mol. structure of teniposide through a structure-guided drug design approach. The IC50 value of novel 4,6-O-thenylidene-β-D-glucopyranoside-(2”-acetamido, 3”-acetyl-di-S-5-fluorobenzothizole/5-fluorobenzoxazole)-4′-demethylepipodophyllotoxin (compounds 15 and 16) was 120.4-125.1μM, which was significantly improved by around 10 times more than teniposide (11.5-22.3μM) against healthy human cells (i.e., HL-7702, H8, MRC-5, and HMEC). In vivo studies demonstrated compounds 15 and 16 significantly suppressed the tumor growth in the HepG2 cell xenograft model without exhibiting obvious toxicity (LD50 values of 208.45 and 167.52 mg/kg), which was lower than that of teniposide (LD50 = 46.12 mg/kg). Compounds 15 and 16 caused mild γH2AX phosphorylation for low DNA toxicity and less inhibition of PI3K/Akt. Compounds 15 and 16 might be potential antitumor drugs with low toxicity.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 13451-78-0 belongs to class benzoxazole, and the molecular formula is C7H4FNOS, Related Products of 13451-78-0.
Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem